Extracts of microalgae and plants for regulating sebum production

ABSTRACT

New extracts of microalgae, halophytes and psammophilous plants are suggested, obtainable by treating said microalgae and plants with a solvent selected from the group consisting of C1-C4 aliphatic alcohols, ethyl acetate, water or their mixtures, removing the dissolved extracts from the residues and recovering the pure extracts from the solvent. The extracts show excellent activity as regulators of the metabolism of human sebaceous glands.

FIELD OF INVENTION

The present invention relates to the area of cosmetics and toiletriesand refers to extracts obtained from microalgae, halophytes living insalt marshes and psammophilous plants living in coastal sand dunes. Theinvention also concerns processes and compositions for obtaining saidextracts, and their use in hair and skin care applications.

STATE OF THE ART

Throughout the last decades, the cosmetics and toiletry industry hasdedicated increasing attention to in the identification of naturalcompounds suitable for use in the preparation of body care products. Theactive ingredients extracted from natural organisms, especially ifobtained with environmentally-friendly methods and without impacting thewild flora and fauna, have represented the higher growth trend in thecosmetics sector for at least 10 years.

This is due to the increased sensibility of consumers to the ethics ofthe green economy, especially in the field of voluptuary goods, but alsoto the awareness that nature houses countless substances withextraordinary beneficial properties, still largely unexploited.Knowledge of natural remedies has been part of the popular culture forcenturies but, in the present time founded on science and technology,this heritage has been almost completely forgotten. However, the conceptthat nature provides cures and therapies promoting the natural defensesof our body is deeply inscribed in our awareness. The present inventionis aimed to provide concrete responses to this request for naturalproducts by the cosmetics producers and consumers.

The growth of the market focused on natural active ingredients has alsoallowed the differentiation of at least two relevant sub-sectors:

-   -   the natural cosmetic products, having formulations based on one        or more natural ingredient,    -   organic products, i.e. products certified as obtained from        compounds and by means of production systems that fully comply        with specific international regulations which govern the        “organic” label.

Research in the field of active ingredients of natural origin istherefore a very relevant and strategic aspect of the production chain,since it provides new compounds and widens the market for the cosmeticsindustry, while promoting “sustainable development” that reconcileseconomic progress with the social responsibility of preserving theplanet's equilibrium.

Plants are the main source of natural active ingredients, on aquantitative basis, with particular reference to antioxidants, vitaminsand micronutrients. Many of these active compounds have been shown toprotect the body from aging processes and environmental damage.Cosmetics have always exploited many natural ingredients obtained fromherbs traditionally known for their beneficial effects, as well asextracts from fruits and vegetables cultivated for food. However, morerecently, many new plants have been introduced in cosmetics as potentialsources of natural active ingredients. In this respect, traditionalChinese medicine has proved an important source of inspiration forresearchers.

The present invention is the result of a great research effort aimed todiscover innovative natural ingredients or extracts suitable to offernatural and safe solutions to some of the skin problems mentionedhereinafter. Some plant and microalgae extracts have unexpectedlydisclosed relevant potential as regulators of the sebaceous glandmetabolism. The results reported here were obtained screening all thepreparations by means of an innovative ex-vivo culture of humansebaceous glands (DE 102013015560.6; Symrise GMBH & Co. KG & CutechSrl). The screening methods usually adopted by cosmetics companies arebased on immortalized lines of sebocytes, which cannot realisticallyreproduce the complex functionality of the complete sebaceous gland.Therefore, since the data reported hereinafter were obtained by treatingex-vivo cultures of human glands, they have to be regarded as the morereliable ones presently achievable with preclinical tests.

Sebaceous glands are microscopic exocrine glands found throughout allareas of the skin except the palms of the hands and soles of the feet.They secret a natural oil, called sebum, which participates with thesweat to compose the hydrolipidic film that covers the skin. Human sebumis a complex mixture of triglycerides, fatty acids, wax esters, sterolesters, cholesterol, cholesterol esters and squalene. Sebum is involvedin epidermal development and barrier maintenance, transportingantioxidants, contributing to mechanical protection, body odor, andgeneration of pheromones. Sebum is directly involved in hormonalsignaling, epidermal differentiation, and protection from ultraviolet(UV) radiation. It cooperates to reduce skin water loss and modulatescomposition and proliferation of the natural micro-flora of the skin.

There are two types of sebaceous glands, those connected to hairfollicles, in pilosebaceous units, and those that exist independently.When they are associated to the hair follicles, one or more glands maysurround each hair follicle, and the glands themselves are surrounded byarrector pili muscles. Sebaceous glands are also found in hairless areas(glabrous skin) of the eyelids (called meibomian glands), nose, penis,labia minora, the inner mucosa of the cheek (Fordyce spots), andnipples.

The overproduction of sebum by sebaceous glands of the scalp is thecause of greasy hair, which is considered a significant aestheticproblem. Many cosmetic treatments, in the form of medicated shampoos andlotions, are proposed to calm the scalp's overproduction of sebum.However, cosmetics companies continuously seek new products, especiallyif obtained from natural ingredients. The seborrhea is involved in theoccurrence of dandruff, a disorder of the scalp characterized by patchesof abundant and loosely adherent flakes, usually accompanied by itching.This accentuated desquamation of the scalp can evolve into seborrheicdermatitis, which is a severe form of dandruff accompanied byinflammation and erythema. The etiology of dandruff and seborrheicdermatitis appears to be dependent upon three factors: sebaceous glandsecretions, micro-flora metabolism, and individual susceptibility. Theregulation of sebum production is therefore a pivotal issue for theprevention of dandruff and seborrheic dermatitis, and the presentinvention is related with this problem, among others.

Undesirable hyperactivity of sebaceous glands can also occur in otherparts of the body, especially on the face. Here the overproduction ofsebum gives the skin a shiny and aesthetically undesirable appearance(oily skin) and can promote other slight blemishes, such as comedones.In some cases, more serious disorders can occur in the presence ofexcessive sebum, such as acne, a skin disease characterized by aninflammatory process of the hair follicle and annexed sebaceous gland.Propionibacterium acnes is considered to be the infectious agent inacne.

P. acnes are aerotolerant anaerobic bacteria that live deep withinfollicles and pores, using sebum, cellular debris and metabolicbyproducts from the surrounding skin tissue as their primary sources ofenergy and nutrients. Elevated production of sebum by hyperactivesebaceous glands or blockage of the follicle can favour P. acnesbacteria proliferation, causing the inflamed pustules (pimples)characteristic of acne. As a consequence, the cosmetics industry isstrongly interested in acquiring compounds suitable to inhibit sebumproduction, especially if this activity is combined with antinflammatoryproperties.

Finally, compounds suitable to regulate sebum production can also findapplication in products for intimate hygiene, since the female externalgenitals have many sebaceous glands. Mons pubis, labia majora, labiaminora and the external side of the vaginal vestibule are rich insebaceous glands and their sebum secretion interacts with the bacterialmicroflora, regulating the pH of the genital area. The fresh sebum doesnot contain significant quantities of free fatty acids, but these arereleased as an effect of the lipases produced by bacteria, inducing theacidification of the genital environment. The regulation of sebum cantherefore represent an important condition for preventing alterations ofthe genital microflora, irritations, itching, etc.

The present invention is the result of a significant effort toinvestigate microalgae strains suitable to be cultivated inphotobioreactors, and plants living in extreme environments, such ashalophytes occurring in salt marshes and psammophilous plants growing onsand dunes of coastal environments.

The plants living in extreme habitats have developed adaptivemetabolites to allow the survival in hostile or stressful conditions.The halophytes living in salt marshes, for instance, must tolerate highlevels of salt in the soil and frequent submersion by the sea tides. Thepsammophilous plants, on the other hand, need to comply with a very dry,nutrient poor and instable soil. The wind action continuously modifiesthe profile of the ground, also producing an erosive effect oneverything that protrudes above its surface. Psammophilous plants havetherefore developed physiological adaptations and protective metabolitessuitable to survive arid conditions, intense solar radiation, hightemperature and abrasion effects due to drifting sand.

Plants growing in salt marshes have already occasionally attracted theattention of cosmetics companies, and some data related to theirexploitation for skin-care products can be found in the prior art. Morethan twenty years ago, FR 2657011 B1 (Secma) claimed the use of Inulaand Salicornia for cosmetic and pharmaceutical preparations withantiradical and antioxidant properties. JP 2010013373 A (Pola Chem Ind.Inc.) refers to preparations obtained from some Chenopodiaceae, amongwhich the halophyte Salicornia europea, for modulating the horny layerof skin in order to improve skin barrier functions. Similarly, JP2005145878 A (Kyoei Chemical Ind. & Kyoei Kagaku Kogyo KK) disclosesskin barrier function restorative/antioxidant/anti-inflammatoryproperties for extracts obtainable from herbs of the genus Salicornia.The far eastern halophyte Salicornia herbacea was extracted forpreparing skin moisturizing products (KR 20020027834 A; Ae Kyung Ind.Co. Ltd.) with anti-wrinkle activity (KR 20110013812 A; Thefaceshop Co.Ltd.) and slimming compositions (KR 20120086438 A, Cosmecca Korea Co.Ltd.).

Less common is the use of psammophilous herbs occurring in marineenvironment as a source of active ingredients for cosmetics. FR2793682B1 (Pierre Fabre Dermo-Cosmetique) suggested the use of Cakile maritimaextracts, a semi-succulent plant on sand dunes and beaches, as aningredient for dermal-cosmetic products and disclosed someexemplificative procedures of extraction. However, this inventionfocuses on the biological activity as moisturizer, while there is noreference to the potential activity of the extracts on the humansebaceous glands. In fact, the whole prior art concerning the herbs thatare the subject of the present invention is totally silent on the use oftheir extracts for the regulation of sebum production.

Among the natural organisms of great interest and only recentlydiscovered by cosmetics, the microalgae occupy a prominent place. Thebiodiversity of microalgae is very high and in great part stilluncertain: to date about 35,000 species of microalgae have beendescribed but the number of unknown species is estimated to vary from200,000 to 800,000. The adaptability of these organisms allows them tosynthesize rare and biologically active compounds suitable to sustainspecific and diversified environmental stresses or to competesuccessfully with other organisms. For instance, many species synthesizecomplex molecules with antibiotic and anticancer properties, some ofwhich have been chemically characterized.

The prior art related to the microalgae exploitation in the field ofcosmetics offers several examples, but very few with regard to theapplication proposed here. The anti-free-radical activity of liquidextracts obtainable from Chlorophyceae, Prasinophyceae, Cryptophyceae,Bacillariophyceae (or diatoms) and Prymnesiophyceae was disclosed in FR2657012 B1 (Secma) in 1990. The exploitability of Chaetoceros forcosmetics products has been known since 1975 thanks to GB 1392131 A(Aubert et al.). Japanese patent JP 3-822959 B2 (Noevir K K) refers toskin lotions effective in preventing skin wrinkles comprising an extractof certain diatoms, particularly Chaetoceros. The extraction solvent isselected from ethanol, methanol, 1,3-butylene glycol, water and is usedin a single form or a two or more mixed form. In a preferredformulation, these solvents include an inorganic salt and a surfactant.U.S. Pat. No. 5,767,095 (Photonz) discloses topical anti-inflammatorycompositions comprising monogalactosyl-dieicosapentanoyl glycerolobtained from Chaetoceros and Thalassiosira, among others. According toEP 1808483 A1 (Cognis) Chlorococcum citriforme has been considered aninteresting source of lutein for cosmetic applications. Internationalpatent application WO 1997/034489 A1 (Aquaculture Technology) refers tothe use of extracts obtained from the marine algae Chaetoceros orThalassiosira as anti-bacterially active agents and to compositionscontaining such agents for use against pathogenic bacteria.International patent application WO 2010/0029115 A1 (LVHM Recherche)proposes the use of certain plant extracts and the microalgaeThalassiosira, for reducing skin and hair pigmentation.

The FR 2894473 A1 (Daniel Jouvance) discloses the use of preparationsobtained from some microalgae (Chromulina, Asterionella and Tetraselmis)for inhibiting the enzymes involved in the metabolism of fatty acids andlipids. Slimming preparations from several species of microalgae areproposed in the Japanese patent JP 2000072642 A1 (Lion). For themicroalgae considered here, several cosmetic applications focused onhair-care, skin-care, antiaging, modulation of skin melanogenesis andsubcutis lipogenesis were disclosed by EP 2629753 A2 (Cutech). The onlyinvention related with the modulation of sebum production is FR 2980698A1 (Gelyma), which refers to the regulation of sebum production obtainedexploiting the combined activity of extracts from the microalgaTetraselmis chui and the macroalga Fucus spiralis.

However, nothing is reported in the prior art on the biologicalproperties of the plants and microalgae considered here as modulators ofsebum production.

DESCRIPTION OF THE INVENTION

In a first embodiment the present invention relates to extracts ofmicroalgae or halophytes or psammophilous plants obtainable by treatingsaid microalgae or plants with a solvent selected from the groupconsisting of C₁-C₄ aliphatic alcohols, ethyl acetate, water or theirmixtures, removing the dissolved extracts from the residues andrecovering the pure extracts from the solvent.

In a second embodiment the present invention also covers a method forobtaining extracts of microalgae or halophytes or psammophilous plantscomprising the following steps:

-   (a) contacting said plant material, optionally minced or crushed or    micronized with a solvent selected from the group consisting of    C₁-C₄ aliphatic alcohols, ethyl acetate, water or their mixtures in    an amount suitable to effect that the actives move into the solvent    phase, optionally at elevated temperatures,-   (b) removing the dissolved extract from the residue, and-   (c) recovering the pure extract from the solvent.

The research conducted unexpectedly revealed that some extractpreparations obtained from different plants and microalgae can beexploited to regulate the sebum synthesis in human sebaceous glands,without exerting any toxic effect. In particular, the object of thepresent invention was to develop new extracts for cosmetic and,respectively, dermatological applications for the regulation of sebumproduction containing:

-   -   lipophilic and hydrophilic extracts obtained from microalgae        belonging to the genus Chlorococcum;    -   lipophilic and hydrophilic extracts obtained from microalgae        belonging to the genus Chaetoceros;    -   lipophilic and hydrophilic extracts obtained from microalgae        belonging to the genus Monodus;    -   lipophilic and hydrophilic extracts obtained from microalgae        belonging to the genus Thalassiosira;    -   lipophilic and hydrophilic extracts obtained from halophytes        belonging to the genus Sarcocornia;    -   lipophilic and hydrophilic extracts obtained from halophytes        belonging to the genus Salicornia;    -   lipophilic and hydrophilic extracts obtained from psammophilous        plants belonging to the genus Inula;    -   lipophilic and hydrophilic extracts obtained from psammophilous        plants belonging to the genus Echinophora.

Chaetoceros sp.

Chaetoceros, belonging to the class of Bacillophyceae, is probably thelargest genus of marine plankton, more particularly diatoms withapproximately 400 species described. Although a large number of thesedescriptions are no longer valid. It is often very difficult todistinguish between different Chaetoceros species. Several attempts havebeen made to restructure this large genus into subgenera and this workis still in progress. However, most of the effort to describe specieshas been focused on boreal areas, and the genus is cosmopolitan, sothere are probably a large number of tropical species still undescribed.The following compilation illustrates suitable strains of Chaetoceroswith respect to the present invention: Chaetoceros abnormis, Chaetocerosaculeatus, Chaetoceros adelianus, Chaetoceros aduncus, Chaetocerosaequatorialis var. antarcticus, Chaetoceros aequatorialis, Chaetocerosaffinis f. pseudosymmetricus, Chaetoceros affinis f. parallelus,Chaetoceros affinis f. inaequalis, Chaetoceros affinis, Chaetocerosamanita, Chaetoceros anastomosans, Chaetoceros angularis, Chaetocerosangulatus, Chaetoceros anostomosans var. speciosus, Chaetoceros armatus,Chaetoceros astrabadicus, Chaetoceros atlanticus var. cornpactus,Chaetoceros atlanticus var. neapolitanus, Chaetoceros atlanticus var.tumescens, Chaetoceros atlanticus, Chaetoceros atlanticus f. audax,Chaetoceros atlanticus var. cruciatus, Chaetoceros audax, Chaetocerosbacteriastrius, Chaetoceros bacteriastroides f. imbricatus, Chaetocerosbacteriastroides, Chaetoceros bermejense, Chaetoceros bisetaceus,Chaetoceros borealis, Chaetoceros borealoides, Chaetoceros breve,Chaetoceros brevis, Chaetoceros brussilowi, Chaetoceros buceros,Chaetoceros buceros, Chaetoceros bulbosus, Chaetoceros bulbosus f.cruciatus, Chaetoceros bulbosus f. schimperana, Chaetoceros bungei,Chaetoceros calcitrans f. pumilus, Chaetoceros californicus, Chaetoceroscapense, Chaetoceros caspicus, Chaetoceros caspicus var. karianus,Chaetoceros caspicus f. pinguichaetus, Chaetoceros castracanei,Chaetoceros castracanei, Chaetoceros ceratospermus var. minor,Chaetoceros ceratosporus var. brachysetus, Chaetoceros ceratosporus,Chaetoceros chunii, Chaetoceros cinctus, Chaetoceros clavigera,Chaetoceros clavigerus, Chaetoceros clevei, Chaetoceros coarctatus,Chaetoceros cochleus, Chaetoceros cornpactus, Chaetoceros cornpressusvar. gracilis, Chaetoceros cornpressus var. hirtisetus, Chaetocerosconcavicorne, Chaetoceros confervoides, Chaetoceros confusus,Chaetoceros constrictus, Chaetoceros convolutus, Chaetoceros convolutusf. trisetosus, Chaetoceros convolutus f. volans, Chaetoceros cornutus,Chaetoceros coronatus, Chaetoceros costatus, Chaetoceros crenatus,Chaetoceros crinitus, Chaetoceros criophilus, Chaetoceros cruciatus,Chaetoceros curvatus, Chaetoceros curvisetus, Chaetoceros dadayi,Chaetoceros danicus, Chaetoceros debilis, Chaetoceros decipiens f.singularis, Chaetoceros decipiens, Chaetoceros delicatulus, Chaetocerosdensus, Chaetoceros diadema, Chaetoceros dichaeta f. unicellularis,Chaetoceros dichaetus, Chaetoceros dichaetus var. polygonus, Chaetocerosdidymus var. praelongus, Chaetoceros didymus f. aestivus, Chaetocerosdidymus f. autumnalis, Chaetoceros didymus, Chaetoceros difficilis,Chaetoceros distichus, Chaetoceros distinguendus, Chaetocerosdiversicurvatus, Chaetoceros diversus var. mediterraneus, Chaetocerosdiversus, Chaetoceros eibenii, Chaetoceros elmorei, Chaetoceroselongatus Chaetoceros exospermus, Chaetoceros externus, Chaetocerosfallax, Chaetoceros femur, Chaetoceros filiferus, Chaetoceros filiforme,Chaetoceros flexuosus, Chaetoceros fragilis Chaetoceros furca var.macroceras, Chaetoceros furcellatus, Chaetoceros fusus, Chaetocerosgalvestonense, Chaetoceros gastridius, Chaetoceros gaussii, Chaetocerosglacialis, Chaetoceros glandazii, Chaetoceros gobii, Chaetocerosgracilis, Chaetoceros grunowii, Chaetoceros hendeyi, Chaetoceroshispidus var. monicae, Chaetoceros hohnii, Chaetoceros holsaticus,Chaetoceros ikari, Chaetoceros imbricatus, Chaetoceros incurvus var.umbonatus, Chaetoceros incurvus, Chaetoceros indicus, Chaetocerosingolfianus, Chaetoceros intermedius, Chaetoceros karianus, Chaetoceroskaryanus, Chaetoceros knipowitschii, Chaetoceros laciniosus, Chaetoceroslaciniosus f. protuberans, Chaetoceros laciniosus f. pelagicus,Chaetoceros lauderi, Chaetoceros leve, Chaetoceros littorale litorale,Chaetoceros lorenzianus var. forceps, Chaetoceros lorenzianus,Chaetoceros malygini, Chaetoceros medius, Chaetoceros meridiana,Chaetoceros mertensii, Chaetoceros messanense, Chaetoceros minimus,Chaetoceros misumensis, Chaetoceros mitra, Chaetoceros muelleri var.duplex, Chaetoceros muelleri var. subsalsum, Chaetoceros muelleri,Chaetoceros muellerii var. subsalsus, Chaetoceros nansenii, Chaetocerosnatatus, Chaetoceros neglectus, Chaetoceros neobulbosus, Chaetocerosneocompactus, Chaetoceros neogracile, Chaetoceros neupokojewii,Chaetoceros nipponicus, Chaetoceros odontella, Chaetoceros okamurae var.tetrasetus, Chaetoceros okamurae, Chaetoceros ostenfeldii, Chaetocerospachtussowii, Chaetoceros pachyceros, Chaetoceros pacificus, Chaetocerosparadoxus, Chaetoceros paradoxus var. luedersii, Chaetoceros parvus,Chaetoceros paulsenii f. robustus, Chaetoceros pavillardii, Chaetocerospelagicus, Chaetoceros pendulus, Chaetoceros perpusillus, Chaetocerosperuvianus var. victoriae, Chaetoceros peruvianus var. gracilis,Chaetoceros peruvianus, Chaetoceros peruvianus var. robustum,Chaetoceros peruvianus var. suadivae, Chaetoceros peruvianus f. volans,Chaetoceros peruvianus f. robustus, Chaetoceros phuketensis, Chaetocerospingue, Chaetoceros pinguichaetus, Chaetoceros pliocenus, Chaetocerosprotuberans, Chaetoceros pseudoaurivillii, Chaetoceros pseudocrinitus,Chaetoceros pseudocurvisetus, Chaetoceros pseudodichaeta, Chaetocerospundulus, Chaetoceros radians Chaetoceros radicans, Chaetocerosrecurvatus f. robustus, Chaetoceros recurvatus, Chaetoceros robustus,Chaetoceros rostratus, Chaetoceros russanowi, Chaetoceros salsugineus,Chaetoceros saltans, Chaetoceros schmidtii, Chaetoceros schuettii f.oceanicus, Chaetoceros secundus, Chaetoceros seiracanthus, Chaetocerossessile, Chaetoceros setoense, Chaetoceros seychellarus, Chaetocerosseychellarus var. austral, Chaetoceros siamense, Chaetoceros similis,Chaetoceros simplex, Chaetoceros skeleton, Chaetoceros socialis f.radians, Chaetoceros socialis, Chaetoceros socialis var. autumnalis,Chaetoceros sedowii, Chaetoceros strictus, Chaetoceros subcompressus,Chaetoceros subsalsus, Chaetoceros subsecundus, Chaetoceros subtilis,Chaetoceros sumatranus, Chaetoceros tenuissimus, Chaetoceros teres f.spinulosus, Chaetoceros teres, Chaetoceros tetrachaeta, Chaetocerostetras, Chaetoceros tetrastichon, Chaetoceros thienemannii, Chaetocerosthrondsenii var. trisetosus, Chaetoceros throndsenii var. throndsenia,Chaetoceros throndsenii, Chaetoceros tortissimus, Chaetocerostransisetus, Chaetoceros vanheurckii, Chaetoceros vermiculus,Chaetoceros villosus, Chaetoceros vistulae, Chaetoceros volans,Chaetoceros weissflogii, Chaetoceros wighamii, Chaetoceros willei,Chaetoceros zachariasi var. longus, Chaetoceros zachariasii var.variatus, Chaetoceros zachariasii var. lotus, Chaetoceros zachariasiiand Chaetoceros ziwolkii.

The preferred strain selected for the present invention is Chaetoceroscalcitrans f. pumilus, a marine strain isolated in 1960 from marinewaters at Urayasu (Chiba Prefecture, Japan) near Umbayashi. This latterone is archived as strain CCAP 1010/11 at the Culture Collection ofAlgae and Protozoa (CCAP) managed by the Scottish Association for MarineScience (also registered in other collections as PLY537; CCMP1315; NEPCC590).

Thalassiosira sp.

Among the various strains of Thalassiosira, also belonging to the classof Bacillariophyceae, Thalassiosira pseudonana is the best known speciesof marine centric diatom. It was chosen as the first eukaryotic marinephytoplankton for whole genome sequencing. T. pseudonana was selectedfor this study because it is a model for diatom physiology studies,belongs to a genus widely distributed throughout the world's oceans, andhas a relatively small genome at 34 mega base pairs. In particular thestrain CS173 obtainable from the Australian CSIRO collection (alsoregistered as CCMP1335 at Provasoli-Guillard National Centre for Cultureof Marine; NEPCC58 at the Canadian Centre for the Culture ofMicroorganisms) is preferably used. This clone was originally collectedin 1958 from Moriches Bay (Long Island, N.Y.) and has been maintainedcontinuously in culture.

Thalassiosira weissflogii is a large diatom (6-20 μm×8-15 μm) that isused in the shrimp and shellfish larviculture industry. This alga isconsidered by several hatcheries to be the single best algae for larvalshrimp. The cell size is 16 fold the biomass of Chaetoceros and 3 foldthe biomass of Tetraselmis. During the winter this algae is about 15microns, but shrinks to about 5 microns during the summer. The color ofTW varies from brown to green to yellow, depending on the amount ofchlorophyll in the culture. This color change does not in any way affectthe quality of the algae.

Other strains of interest for and suitable to be considered as source ofbiological material for the present invention include the following:Thalassiosira aff. antarctica, Thalassiosira antarctica, Thalassiosiradecipiens, Thalassiosira eccentrica, Thalassiosira floridana,Thalassiosira gravida, Thalassiosira guillardii, Thalassiosira hyalina,Thalassiosira minima, Thalassiosira nordenskioeldii, Thalassiosiraoceanica, Thalassiosira oestrupii, Thalassiosira punctigera,Thalassiosira rotula and Thalassiosira tumida. All these strains ofThalassiosira are suitable as starting materials in order to obtain theextracts according to the present invention.

Monodus sp.

Monodus sp., belonging to the class Eustigmatophyceae, is a class ofmicroalgae rich in polyunsaturated fatty acids. The preferred strain isMonodus subterraneus (also known as Monodus. subterranea) and inparticular the strain CCAP 848/1 obtainable from the Culture Collectionof Algae and Protozoa managed by the Scottish Association for MarineScience (also registered as ATCC 30593; UTEX 151 and SAG 848-1) ispreferably used.

Other strains of interest for and suitable to be considered as source ofbiological material for the present invention include the following:Monodus subterranea majus, Monodus acuminata, Monodus amicimei, Monoduschodatii, Monodus coccomyxa, Monodus coccomyxoides, Monodus cystiformis,Monodus fusiformis, Monodus guttula, Monodus pyreniger, Monodussubglobosa, Monodus subsalsus and Monodus unipapilla.

Chlorococcum sp.

Chlorococcum is a genus of algae, in the Chlorococcaceae family. Thefollowing compilation illustrates suitable strains of Chlorococcum withrespect to the present invention: Chlorococcum acidum, Chlorococcumaegyptiacum, Chlorococcum botryoides, Chlorococcum choloepodis,Chlorococcum citriforme, Chlorococcum costatozygotum, Chlorococcumdiplobionticum, Chlorococcum dissectum, Chlorococcum echinozygotum,Chlorococcum elbense, Chlorococcum elkhartiense, Chlorococcumellipsoideum, Chlorococcum hypnosporum, Chlorococcum infusionum,Chlorococcum isabeliense, Chlorococcum lobatum, Chlorococcummacrostigmatum, Chlorococcum minimum, Chlorococcum minutum, Chlorococcumnovaeangliae, Chlorococcum oleofaciens, Chlorococcum olivaceum,Chlorococcum pamirum, Chlorococcum pinguideum, Chlorococcum polymorphum,Chlorococcum pseudodictyosphaerium, Chlorococcum pyrenoidosum,Chlorococcum refringens, Chlorococcum salinum, Chlorococcumschizochlamys, Chlorococcum schwarzii, Chlorococcum submarinum,Chlorococcum tatrense and Chlorococcum vacuolatum.

The preferred strain selected for the present invention is Chlorococcumminutum, archived as strain CCAP 213/7 (SAG 213-7; SAG 21.95; UTEX 117;CCAO 290) at the Culture Collection of Algae and Protozoa (CCAP) managedby the Scottish Association for Marine Science. This latter was isolatedby Bold from soil in India.

Salicornia sp.

Salicornia is a widely distributed salt-marsh plant with fleshyscalelike leaves, belonging to the Chenopodiaceae family (orAmaranthaceae according to an alternative taxonomical classification).It is also known by the popular name “glasswort” because in medieval andearly post-medieval times the ashes of the burned plant were exploitedin glassmaking due to their high alkali content.

Many species of Salicornia can be used as an ingredient for the presentinvention, however, the preferred species are Salicornia europaea(common glasswort) and Salicornia veneta, endemic to the North Adriaticand very common in the lagoon of Venice. Salicornia is highly edible,either cooked or raw. Other species suitable to be exploited as materialsource for the present invention are: Salicornia bigelovii (dwarfglasswort), Salicornia depressa, Salicornia dolichostachya, Salicorniaemerici, Salicornia herbacea, Salicornia maritima (slender glasswort),Salicornia nitens, Salicornia obscura, Salicornia patula, Salicorniaprostrata, Salicornia pusilla, Salicornia ramosissima (purple glasswort)and Salicornia rubra.

The genus Salicornia and the following genus Sarcocornia comprise veryhomogeneous species from a morphological, ecological and systematicpoint of view. They are expected to show similar biological propertiesalso for the applications proposed here.

Sarcocornia sp.

This plant is very similar to the previous one and both are generallygrouped under the name glasswort. However, the genus Sarcocorniacomprises perennial halophytes occurring in middle and high tidal marshzones, salt or brackish marshes; also diked nontidal seasonal salinewetlands. Sarcocornia was formed from species formerly belonging toSalicornia and Arthrocnemum, however, the taxonomy of this genus isdifficult and specialists have no a univocal interpretation.

The preferred species for preparing the extracts object of thisinvention is Sarcocornia fruticosa, however, many other species can beconsidered as source of biological material for the present invention.These include: Sarcocornia alpini, Sarcocornia ambigua, Sarcocorniablackiana (thick-head glasswort), Sarcocornia capensis, Sarcocorniadecumbens, Sarcocornia globosa, Sarcocornia littorea, Sarcocorniamagellanica, Sarcocornia mossiana, Sarcocornia natalensis, Sarcocornianeei, Sarcocornia obclavata, Sarcocornia pacifica (=Salicorniavirginica) (Pacific swampfire, Pacific glasswort), Sarcocornia perennis(chickenclaws, perennial glasswort, Virginia glasswort), Sarcocorniapillansii, Sarcocornia pulvinata, Sarcocornia quinqueflora (Australiansamphire), Sarcocornia quinqueflora ssp. quinqueflora, Sarcocorniaquinqueflora ssp. tasmanica, Sarcocornia terminalis, Sarcocorniautahensis (Utah swampfire) and Sarcocornia xerophila.

Inula sp.

Inula is a large genus of about 90 species of flowering plants in theAsteraceae family, many of which are commonly cultivated as gardenflowers. Inula (=Limbarda) crithmoides, also known as golden samphire,is a Eurasian perennial coastal species, which may be found growing onsea-cliff ledges, salt marshes or coastal sandy beaches and dunes. Youngleaves may be eaten raw or cooked as a leaf vegetable. It is verytolerant to salt, and can grow on light (sandy), medium (loamy) andheavy (clay) soils, however, it prefers well-drained soil. It shows abushy habit and has semi-succulent leaves.

Inula crithmoides is the preferred species for the present invention,however, other species can be considered as source of biologicalmaterial for the present invention, including the following: Inulaacaulis (stemless inula), Inula acervata, Inula acinacifolia, Inulaacuminata, Inula afghanica, Inula anatolica, Inula auriculata, Inulabifrons, Inula britannica (British yellowhead), Inula candida, Inulacappa, Inula caspica, Inula clarkei, Inula conyzae, Inula cuspidata,Inula ensifolia, Inula eupatorioides, Inula falconeri, Inula forrestii,Inula germanica, Inula grandis, Inula helenioides, Inula helenium, Inulahelianthus-aquatica, Inula helvetica, Inula hirta, Inula hookeri, Inulahupehensis, Inula japonica, Inula koelzii, Inula lineariifolia, Inulamagnifica, Inula montana, Inula multicaulis, Inula nervosa, Inulaobtusifolia, Inula oculus-christi, Inula orientalis, Inula pterocaula,Inula racemosa, Inula rhizocephala, Inula rhizocephaloides, Inularubricaulis, Inula salicina (Irish fleabane, willowleaf yellowhead),Inula salsoloides, Inula sericophylla, Inula spiraeifolia, Inulastewartii, Inula subfloccosa, Inula thapsoides, Inula verbascifolia andInula wissmanniana.

Echinophora sp.

This genus belongs to the Apiaceae family (or Umbelliferae) andcomprises several species occurring in coastal sandy environments. Somespecies are known for their therapeutic properties, e.g. E. platylobaoccurring in Iran. Echinophora sibthorpiana or Echinophora tenuifoliaare sometimes used as a flavoring in tarhana, a middle-eastern dishbased on a fermented mixture of grains and yoghurt or fermented milk.

The species of most interest for the present invention is E. spinosa, aperennial semi-succulent herb up to 60-70 cm tall, growing on coastalsand dunes of the Mediterranean. The aerial part dies in winter, but theunderground rhizome survives, developing up to 1 m in length. Stems areerect, robust and branched, grayish-green in color. The leaves aresparse and rigid, deeply divided in stingray lobes, inferiorly keeled,terminating with a pungent rigid spine. The inflorescence has 6-10 raysand is positioned at the top of the stem.

However, other species can be considered as potential source ofbiological material for the present invention: Echinophora carvifolia,Echinophora chrysantha, Echinophora cinerea, Echinophora lamondiana,Echinophora orientalis, Echinophora platyloba, Echinophora scabra,Echinophora tenuifolia, Echinophora tournefortii and Echinophoratrichophylla.

Extraction Process of Microalgae

Another object of the present invention relates to a process forobtaining the extracts adopted for the experimental activities. Themicroalgal biomass can be obtained by cultivation in photobioreactors orin large polyethylene bags or tanks, under daylight or artificial light.The cultivation can occur indoors or outdoors. Some microalgal strainscan be also cultivated in heterotrophic conditions, in the dark, inappropriate bioreactors.

When the microalgal biomass reaches a suitable cell density, it can beharvested by centrifugation or sedimentation or flocculation or withother techniques suitable to preserve the integrity of the cellmaterial. The harvested biomass is freeze dried and packaged in vacuumsealed plastic bags or aluminum foil bags, then frozen and preserved at−20° C. till the time of extraction.

Basically, the extracts according to the present invention may beprepared by methods known per se, for example, by aqueous, organic oraqueous/organic extraction of the microalgae using the solventsexplained hereinafter. Suitable extraction processes are anyconventional extraction processes such as maceration, re-maceration,digestion, agitation maceration, vortex extraction, ultrasonicextraction, counter current extraction, percolation, re-percolation,evacolation (extraction under reduced pressure), diacolation andsolid/liquid extraction under continuous reflux. Percolation isadvantageous for industrial uses. Any size reduction methods known tothe expert, for example, freeze grinding, may be used. Preferredsolvents for the extraction process are methanol, ethanol, isopropylalcohol, ethyl acetate, hexane and water (preferably hot water with atemperature above 80° C., and more particularly above 95° C.) ormixtures of said organic solvents and water, more particularly, lowmolecular weight alcohols with more or less high water contents. Anextraction with methanol, ethanol and water-containing mixtures thereofis particularly preferred. The extraction process is generally carriedout at temperatures of from about 10 to about 100° C. In one preferredembodiment, the extraction process is carried out in an inert gasatmosphere to avoid the oxidation of the ingredients of the extract.This is particularly important where extraction is carried out attemperatures above 40° C. The extraction times are selected by theexpert depending on the starting material, the extraction process, theextraction temperature, and the ratio of solvent to raw material, etc.After the extraction process, the crude extracts obtained may optionallybe subjected to other typical steps, such as, for example, purification,concentration and/or decoloration. If desired, the extracts thusprepared may be subjected, for example, to the selective removal ofindividually unwanted ingredients. The extraction process may be carriedout to any degree, but is usually continued to exhaustion. Typicalyields (=extract dry matter based on the quantity of raw material used)in the extraction of the starting materials are of the order of fromabout 1 to about 50%, preferably from about 2 to about 20%, and morepreferably from about 5 to about 15% b.w.—calculated on the startingmaterials.

In the following, the typical process for obtaining the microalgaeextracts according to the invention is described in more detail:

-   -   Each gram of dry biomass was extracted by treatment with 100 ml        of solvent, stirring the suspension at room temperature for 16        hours in the dark;    -   the residual cell material was separated from the extract by        centrifugation at 2000 G for 15 minutes;    -   the residual biomass was washed by suspending it in 50 ml of        solvent;    -   the cell material was separated from the washing solvent by        centrifugation at 2000 G for 15 minutes;    -   the residual biomass was washed again by suspending it in 50 ml        of solvent;    -   the cell material was separated from the washing solvent by        centrifugation at 2000 G for 15 minutes;    -   the firstly collected extract and the washing solvent volumes        were mixed, and the resulting extract was considered to have a        conventional concentration of 5000 μg/ml (1000 mg of dry algae        in 200 ml of solvent).

According to the present invention, cell material of the aforementionedmicroalgae was extracted with a liquid extractant selected from thegroup consisting of ethyl acetate, isopropanol, ethanol, methanol andwater.

The extractant can also comprise a mixture of two or more of theaforementioned solvents. Hereinafter, the microalgae extractconcentrations will be conventionally expressed as the ratio between thequantity (in weight) of cell material treated and the extractive solvent(in volume). For instance, by treating 1 g of dry powered microalgaewith 200 ml of extractive solvent, 200 ml of extract at 5000 μg/ml (w/v)are obtained without regard for the quantity of compounds reallysolubilised in the solvent. This conventional concentration allows torepresent the quantity of dried microalgae effectively required toproduce the experimental results described. However, the estimated dryweights of the extracts are reported in Table 1 and the real extractconcentration can be calculated. As the composition of the microalgaemay change in relation to culture methods and environmental conditions,also the extraction efficacy may change and the extract dry weights haveto be considered as raw indications.

Quantity and quality of compounds present in the extracts may vary withrespect to both solvent properties and preparation protocol. Theselected algae strains showed a different refractoriness to releasesubstances under action of the solvent, basically depending on thecharacteristics of their respective cell wall. In Table 1, the dryweights of the prepared extracts expressed as percentage of the relatedintegral microalgae material are reported:

TABLE 1 Dry weight of the extracts expressed as percentage of the drycell material Chaetoceros calcitrans Thalassiosira Monodus ChlorococcumExtract code f. pumilus pseudonana subterraneus minutum Methanol 54% 39%  20% 24% Ethanol 22% 27% 7-10% 16% Isopropyl 10% 15%  6-9% 10% alcoholEthyl acetate 9-12%   18%   4% 5-8%  Water 64% 22%   26% 22%

Extraction Process of Terrestrial Plants

The biological material submitted to extraction can include both epigealand/or hypogeal parts of the plants. This material can be harvested,rapidly freeze-dried and then finely grinded and extracted following thesame process described for microalgae.

However, for the experimental program which led to the presentinvention, the plants were submitted to extraction freshly harvested.The extraction process consisted of the following steps:

-   -   finely grinding parts of the freshly harvested plant using        electromechanical devices, blades suitable for manual use or any        other methods,    -   homogenizing this minced material pounding it in a mortar        together with an extraction solvent selected from the group        consisting of C₁-C₄ aliphatic alcohols, ethyl acetate, water or        their mixtures in an amount suitable to effect that the actives        move into the solvent phase, optionally at elevated        temperatures,    -   removing the dissolved extract from the residue, and    -   recovering the pure extract from the solvent.

Basically, the extracts according to the present invention may beprepared by methods known per se, for example, by aqueous, organic oraqueous/organic extraction of the plants using the solvents explainedabove. Suitable extraction processes are any conventional extractionprocesses such as maceration, re-maceration, digestion, agitationmaceration, vortex extraction, ultrasonic extraction, counter currentextraction, percolation, repercolation, evacolation (extraction underreduced pressure), diacolation and solid/liquid extraction undercontinuous reflux. Percolation is advantageous for industrial uses. Anysize reduction methods known to the expert, for example, freezegrinding, may be used. Preferred solvents for the extraction process aremethanol, ethanol, isopropyl alcohol, ethyl acetate and water(preferably hot water with a temperature above 80° C., and moreparticularly above 95° C.) or mixtures of said organic solvents andwater, more particularly, low molecular weight alcohols with more orless high water contents. An extraction with methanol, ethanol andwater-containing mixtures thereof is particularly preferred. Theextraction process is generally carried out at temperatures of fromabout 20 to about 100° C., and preferably from about 50 to about 70° C.In one preferred embodiment, the extraction process is carried out in aninert gas atmosphere to avoid the oxidation of the ingredients of theextract. This is particularly important where extraction is carried outat temperatures above 40° C. The extraction times are selected by theexpert depending on the starting material, the extraction process, theextraction temperature, and the ratio of solvent to raw material, etc.After the extraction process, the crude extracts obtained may optionallybe subjected to other typical steps, such as, for example, purification,concentration and/or decoloration. If desired, the extracts thusprepared may be subjected, for example, to the selective removal ofindividually unwanted ingredients. The extraction process may be carriedout to any degree, but is usually continued to exhaustion. Typicalyields (=extracted dry matter based on the quantity of raw freshmaterial used) in the extraction of the starting materials are of theorder of from about 1 to about 20%, preferably from about 1 to about10%, and more preferably from about 2 to about 6% b.w.—calculated on thestarting materials. The extraction is preferably performed on freshlyharvested plants, but also frozen or lyophilized material can be used.

In the following, the processes for obtaining the extracts according tothe invention is described in more detail:

Water or Methanol or Ethanol or Isopropyl Alcohol or Ethyl AcetateExtraction Process: Single Solvent Extraction

-   -   Each gram of fresh minced and macerated plant was extracted by        treatment with 4 ml of solvent, stirring the suspension at room        temperature for 16 hours in the dark;    -   the residual material was separated from the extract by        centrifugation at 2000 G for 15 minutes;    -   the residual material was washed by suspending it in 0.5 ml of        solvent;    -   the cell material was separated from the washing solvent by        centrifugation at 2000 G for 15 minutes;    -   the residual biomass was washed again by suspending it in 0.5 ml        of solvent;    -   the cell material was separated from the washing solvent by        centrifugation at 2000 G for 15 minutes;    -   the firstly collected extract and the washing solvent volumes        were mixed obtaining the final extract,    -   a sample of extract has been evaporated from the solvent in        order to weight the dry residual and estimate its concentration.

Extracts can be obtained adopting the protocol above reported also usingmixture of the cited solvents. It has to be considered that, workingwith fresh biomass, alcoholic solvents produce a hydro-alcoholicextract, since the alcoholic solvent determines the extraction of thetissue water over that of the plant components preferentially soluble inalcohol. However, this does not occur in case of solvent immiscible withwater, e.g. by using ethyl acetate.

In order to obtain extracts strictly composed by substances selected inbase to the affinity for the extractive solvent, it is recommendable toprocess freeze-dried biomasses.

Differently from what said for the extracts prepared from microalgae,the dry weight of the plant extracts was estimated in order to calculateexactly their concentration in the experimental treatments of theexamples hereinafter reported.

Industrial Application

Another object of the present invention is directed at cosmetic andpersonal care compositions comprising extracts of microalgae or plantsand a cosmetically acceptable carrier selected from the group consistingof C₁-C₄ aliphatic alcohols, polyols having 3 to 12 carbon atoms, oilcomponents, water and their mixtures. Suitable carriers encompass, forexample, ethanol, propanol, isopropyl alcohol, all isomeric forms ofbutanol, ethylene and/or propylene glycol and its dimers and trimers,glycerol, glucose, pentaerythritol and the like. Suitable oil componentsare disclosed in the following chapter.

The compositions may contain the extracts in amounts of from 0.00001 to50, preferably from 0.01 to 20, and more preferably from 0.1 to 10%b.w.—the amounts calculated on the dry matter of the extracts. Theremaining parts are the carriers. Typically, the administration of theextracts takes place topically; however, it is also possible to use theextracts—especially after encapsulation—for oral uptake.

Cosmetic or Personal Care Composition

Another object of the present invention encompasses a cosmetic orpersonal care composition comprising said aromatic nitriles and saidperfumery grade solvents. The cosmetic or personal care composition mayrepresent a skin care, hair care and/or sun care product, such as forexample a cosmetic cream, lotion, spray, emulsion, ointment, gel ormouse and the like. Typical examples are skin creams and hair shampoos,antiperspirants and soaps.

The preparations according to the invention may contain abrasives,anti-acne agents, agents against ageing of the skin, anti-cellulitisagents, antidandruff agents, anti-inflammatory agents,irritation-preventing agents, irritation-inhibiting agents,antioxidants, astringents, perspiration-inhibiting agents, antisepticagents, ant-statics, binders, buffers, carrier materials, chelatingagents, cell stimulants, cleansing agents, care agents, depilatoryagents, surface-active substances, deodorizing agents, antiperspirants,softeners, emulsifiers, enzymes, essential oils, fibres, film-formingagents, fixatives, foam-forming agents, foam stabilizers, substances forpreventing foaming, foam boosters, gelling agents, gel-forming agents,hair care agents, hair-setting agents, hair-straightening agents,moisture-donating agents, moisturizing substances, moisture-retainingsubstances, bleaching agents, strengthening agents, stain-removingagents, optically brightening agents, impregnating agents,dirt-repellent agents, friction-reducing agents, lubricants,moisturizing creams, ointments, opacifying agents, plasticizing agents,covering agents, polish, gloss agents, polymers, powders, proteins,re-oiling agents, abrading agents, silicones, skin-soothing agents,skin-cleansing agents, skin care agents, skin-healing agents,skin-lightening agents, skin-protecting agents, skin-softening agents,hair promotion agents, cooling agents, skin-cooling agents, warmingagents, skin-warming agents, stabilizers, UV-absorbing agents, UVfilters, detergents, fabric conditioning agents, suspending agents,skin-tanning agents, thickeners, vitamins, oils, waxes, fats,phospholipids, saturated fatty acids, mono- or polyunsaturated fattyacids, α-hydroxy acids, polyhydroxyfatty acids, liquefiers, dyestuffs,colour-protecting agents, pigments, anti-corrosives, aromas, flavouringsubstances, odoriferous substances, polyols, surfactants, electrolytes,organic solvents or silicone derivatives and the like as additionalauxiliaries and additives.

Surfactants

Preferred auxiliaries and additives are anionic and/or amphoteric orzwitterionic surfactants. Typical examples of anionic surfactants aresoaps, alkyl benzenesulfonates, alkanesulfonates, olefin sulfonates,alkylether sulfonates, glycerol ether sulfonates, methyl estersulfonates, sulfofatty acids, alkyl sulfates, fatty alcohol ethersulfates, glycerol ether sulfates, fatty acid ether sulfates, hydroxymixed ether sulfates, monoglyceride (ether) sulfates, fatty acid amide(ether) sulfates, mono- and dialkyl sulfosuccinates, mono- and dialkylsulfosuccinamates, sulfotriglycerides, amide soaps, ether carboxylicacids and salts thereof, fatty acid isethionates, fatty acidsarcosinates, fatty acid taurides, N-acylamino acids such as, forexample, acyl lactylates, acyl tartrates, acyl glutamates and acylaspartates, alkyl oligoglucoside sulfates, protein fatty acidcondensates (particularly wheat-based vegetable products) and alkyl(ether) phosphates. If the anionic surfactants contain polyglycol etherchains, they may have a conventional homolog distribution although theypreferably have a narrow-range homolog distribution. Typical examples ofamphoteric or zwitterionic surfactants are alkylbetaines,alkylamidobetaines, aminopropionates, aminoglycinates, imidazoliniumbetaines and sulfobetaines. The surfactants mentioned are all knowncompounds. Information on their structure and production can be found inrelevant synoptic works, cf. for example J. Falbe (ed.), “Surfactants inConsumer Products”, Springer Verlag, Berlin, 1987, pages 54 to 124 or J.Falbe (ed.), “Katalysatoren, Tenside and Mineralöladditive (Catalysts,Surfactants and Mineral Oil Additives)”, Thieme Verlag, Stuttgart, 1978,pages 123-217. The percentage content of surfactants in the preparationsmay be from 0.1 to 10% by weight and is preferably from 0.5 to 5% byweight, based on the preparation.

Oil Bodies

Suitable oil bodies, which form constituents of the O/W emulsions, are,for example, Guerbet alcohols based on fatty alcohols having 6 to 18,preferably 8 to 10, carbon atoms, esters of linear C₆-C₂₂-fatty acidswith linear or branched C₆-C₂₂-fatty alcohols or esters of branchedC₆-C₁₃-carboxylic acids with linear or branched C₆-C₂₂-fatty alcohols,such as, for example, myristyl myristate, myristyl palmitate, myristylstearate, myristyl isostearate, myristyl oleate, myristyl behenate,myristyl erucate, cetyl myristate, cetyl palmitate, cetyl stearate,cetyl isostearate, cetyl oleate, cetyl behenate, cetyl erucate, stearylmyristate, stearyl palmitate, stearyl stearate, stearyl isostearate,stearyl oleate, stearyl behenate, stearyl erucate, isostearyl myristate,isostearyl palmitate, isostearyl stearate, isostearyl isostearate,isostearyl oleate, isostearyl behenate, isostearyl oleate, oleylmyristate, oleyl palmitate, oleyl stearate, oleyl isostearate, oleyloleate, oleyl behenate, oleyl erucate, behenyl myristate, behenylpalmitate, behenyl stearate, behenyl isostearate, behenyl oleate,behenyl behenate, behenyl erucate, erucyl myristate, erucyl palmitate,erucyl stearate, erucyl isostearate, erucyl oleate, erucyl behenate anderucyl erucate. Also suitable are esters of linear C₆-C₂₂-fatty acidswith branched alcohols, in particular 2-ethylhexanol, esters ofC₁₈-C₃₈-alkylhydroxy carboxylic acids with linear or branchedC₆-C₂₂-fatty alcohols, in particular Dioctyl Malate, esters of linearand/or branched fatty acids with polyhydric alcohols (such as, forexample, propylene glycol, dimerdiol or trimertriol) and/or Guerbetalcohols, triglycerides based on C₆-C₁₀-fatty acids, liquidmono-/di-/triglyceride mixtures based on C₆-C₁₈-fatty acids, esters ofC₆-C₂₂-fatty alcohols and/or Guerbet alcohols with aromatic carboxylicacids, in particular benzoic acid, esters of C₂-C₁₂-dicarboxylic acidswith linear or branched alcohols having 1 to 22 carbon atoms or polyolshaving 2 to 10 carbon atoms and 2 to 6 hydroxyl groups, vegetable oils,branched primary alcohols, substituted cyclohexanes, linear and branchedC₆-C₂₂-fatty alcohol carbonates, such as, for example, DicaprylylCarbonate (Cetiol® CC), Guerbet carbonates, based on fatty alcoholshaving 6 to 18, preferably 8 to 10, carbon atoms, esters of benzoic acidwith linear and/or branched C₆-C₂₂-alcohols (e.g. Finsolv® TN), linearor branched, symmetrical or asymmetrical dialkyl ethers having 6 to 22carbon atoms per alkyl group, such as, for example, dicaprylyl ether(Cetiol® OE), ring-opening products of epoxidized fatty acid esters withpolyols, silicone oils (cyclomethicones, silicone methicone grades,etc.) and/or aliphatic or naphthenic hydrocarbons, such as, for example,squalane, squalene or dialkylcyclohexanes.

Emulsifiers

Other surfactants may also be added to the preparations as emulsifiers,including for example:

-   -   products of the addition of 2 to 30 mol ethylene oxide and/or 0        to 5 mol propylene oxide onto linear C₈₋₂₂ fatty alcohols, onto        C₁₂₋₂₂ fatty acids and onto alkyl phenols containing 8 to 15        carbon atoms in the alkyl group;    -   C_(12/18) fatty acid monoesters and diesters of addition        products of 1 to 30 mol ethylene oxide onto glycerol;    -   glycerol mono- and diesters and sorbitan mono- and diesters of        saturated and unsaturated fatty acids containing 6 to 22 carbon        atoms and ethylene oxide addition products thereof;    -   addition products of 15 to 60 mol ethylene oxide onto castor oil        and/or hydrogenated castor oil;    -   polyol esters and, in particular, polyglycerol esters such as,        for example, polyglycerol polyricinoleate, polyglycerol        poly-12-hydroxystearate or polyglycerol dimerate isostearate.        Mixtures of compounds from several of these classes are also        suitable;    -   addition products of 2 to 15 mol ethylene oxide onto castor oil        and/or hydrogenated castor oil;    -   partial esters based on linear, branched, unsaturated or        saturated C_(6/22) fatty acids, ricinoleic acid and        12-hydroxystearic acid and glycerol, polyglycerol,        pentaerythritol, -dipentaerythritol, sugar alcohols (for example        sorbitol), alkyl glucosides (for example methyl glucoside, butyl        glucoside, lauryl glucoside) and polyglucosides (for example        cellulose);    -   mono-, di and trialkyl phosphates and mono-, di- and/or        tri-PEG-alkyl phosphates and salts thereof;    -   wool wax alcohols;    -   polysiloxane/polyalkyl polyether copolymers and corresponding        derivatives;    -   mixed esters of pentaerythritol, fatty acids, citric acid and        fatty alcohol and/or mixed esters of C₆₋₂₂ fatty acids, methyl        glucose and polyols, preferably glycerol or polyglycerol,    -   polyalkylene glycols and    -   glycerol carbonate.

The addition products of ethylene oxide and/or propylene oxide ontofatty alcohols, fatty acids, alkylphenols, glycerol mono- and diestersand sorbitan mono- and diesters of fatty acids or onto castor oil areknown commercially available products. They are homologue mixtures ofwhich the average degree of alkoxylation corresponds to the ratiobetween the quantities of ethylene oxide and/or propylene oxide andsubstrate with which the addition reaction is carried out. C_(12/18)fatty acid monoesters and diesters of addition products of ethyleneoxide onto glycerol are known as lipid layer enhancers for cosmeticformulations. The preferred emulsifiers are described in more detail asfollows:

Partial glycerides. Typical examples of suitable partial glycerides arehydroxystearic acid monoglyceride, hydroxystearic acid diglyceride,isostearic acid monoglyceride, isostearic acid diglyceride, oleic acidmonoglyceride, oleic acid diglyceride, ricinoleic acid monoglyceride,ricinoleic acid diglyceride, linoleic acid monoglyceride, linoleic aciddiglyceride, linolenic acid monoglyceride, linolenic acid diglyceride,erucic acid monoglyceride, erucic acid diglyceride, tartaric acidmonoglyceride, tartaric acid diglyceride, citric acid monoglyceride,citric acid diglyceride, malic acid monoglyceride, malic aciddiglyceride and technical mixtures thereof which may still contain smallquantities of triglyceride from the production process. Additionproducts of 1 to 30 and preferably 5 to 10 mol ethylene oxide onto thepartial glycerides mentioned are also suitable.

Sorbitan esters. Suitable sorbitan esters are sorbitan monoisostearate,sorbitan sesquiisostearate, sorbitan diisostearate, sorbitantriisostearate, sorbitan monooleate, sorbitan sesquioleate, sorbitandioleate, sorbitan trioleate, sorbitan monoerucate, sorbitansesquierucate, sorbitan dierucate, sorbitan trierucate, sorbitanmonoricinoleate, sorbitan sesquiricinoleate, sorbitan diricinoleate,sorbitan triricinoleate, sorbitan monohydroxystearate, sorbitansesquihydroxystearate, sorbitan dihydroxystearate, sorbitantrihydroxystearate, sorbitan monotartrate, sorbitan sesquitartrate,sorbitan ditartrate, sorbitan tritartrate, sorbitan monocitrate,sorbitan sesquicitrate, sorbitan dicitrate, sorbitan tricitrate,sorbitan monomaleate, sorbitan sesquimaleate, sorbitan dimaleate,sorbitan trimaleate and technical mixtures thereof. Addition products of1 to 30 and preferably 5 to 10 mol ethylene oxide onto the sorbitanesters mentioned are also suitable.

Polyglycerol esters. Typical examples of suitable polyglycerol estersare Polyglyceryl-2 Dipolyhydroxystearate (Dehymuls® PGPH),Polyglycerin-3-Diisostearate (Lameform® TGI), Polyglyceryl-4 Isostearate(Isolan® GI 34), Polyglyceryl-3 Oleate, Diisostearoyl Polyglyceryl-3Diisostearate (Isolan® PDI), Polyglyceryl-3 Methylglucose Distearate(Tego Care® 450), Polyglyceryl-3 Beeswax (Cera Bellina®), Polyglyceryl-4Caprate (Polyglycerol Caprate T2010/90), Polyglyceryl-3 Cetyl Ether(Chimexane® NL), Polyglyceryl-3 Distearate (Cremophor® GS 32)® andPolyglyceryl Polyricinoleate (Admul® WOL 1403), Polyglyceryl DimerateIsostearate and mixtures thereof. Examples of other suitablepolyolesters are the mono-, di- and triesters of trimethylol propane orpentaerythritol with lauric acid, cocofatty acid, tallow fatty acid,palmitic acid, stearic acid, oleic acid, behenic acid and the likeoptionally reacted with 1 to 30 mol ethylene oxide.

Anionic emulsifiers. Typical anionic emulsifiers are aliphatic C₁₂₋₂₂fatty acids, such as palmitic acid, stearic acid or behenic acid forexample, and C₁₂₋₂₂ dicarboxylic acids, such as azelaic acid or sebacicacid for example.

Amphoteric emulsifiers. Other suitable emulsifiers are amphoteric orzwitterionic surfactants. Zwitterionic surfactants are surface-activecompounds which contain at least one quaternary ammonium group and atleast one carboxylate and one sulfonate group in the molecule.Particularly suitable zwitterionic surfactants are the so-calledbetaines, such as the N-alkyl-N,N-dimethyl ammonium glycinates, forexample cocoalkyl dimethyl ammonium glycinate,N-acylaminopropyl-N,N-dimethyl ammonium glycinates, for examplecocoacylaminopropyl dimethyl ammonium glycinate, and2-alkyl-3-carboxymethyl-3-hydroxyethyl imidazolines containing 8 to 18carbon atoms in the alkyl or acyl group and cocoacylaminoethylhydroxyethyl carboxymethyl glycinate. The fatty acid amide derivativeknown under the CTFA name of Cocamidopropyl Betaine is particularlypreferred. Ampholytic surfactants are also suitable emulsifiers.Ampholytic surfactants are surface-active compounds which, in additionto a C_(8/18) alkyl or acyl group, contain at least one free amino groupand at least one —COOH— or —SO₃H— group in the molecule and which arecapable of forming inner salts. Examples of suitable ampholyticsurfactants are N-alkyl glycines, N-alkyl propionic acids,N-alkylaminobutyric acids, N-alkyliminodipropionic acids,N-hydroxyethyl-N-alkylamidopropyl glycines, N-alkyl taurines, N-alkylsarcosines, 2-alkylaminopropionic acids and alkylaminoacetic acidscontaining around 8 to 18 carbon atoms in the alkyl group. Particularlypreferred ampholytic surfactants are N-cocoalkylaminopropionate,cocoacylaminoethyl aminopropionate and C_(12/18) acyl sarcosine.

Superfatting Agents and Consistency Factors

Superfatting agents may be selected from such substances as, forexample, lanolin and lecithin and also polyethoxylated or acylatedlanolin and lecithin derivatives, polyol fatty acid esters,monoglycerides and fatty acid alkanolamides, the fatty acidalkanolamides also serving as foam stabilizers.

The consistency factors mainly used are fatty alcohols or hydroxyfattyalcohols containing 12 to 22 and preferably 16 to 18 carbon atoms andalso partial glycerides, fatty acids or hydroxyfatty acids. Acombination of these substances with alkyl oligoglucosides and/or fattyacid N-methyl glucamides of the same chain length and/or polyglycerolpoly-12-hydroxystearates is preferably used.

Thickening Agents and Rheology Additives

Suitable thickeners are polymeric thickeners, such as Aerosil® types(hydrophilic silicas), polysaccharides, more especially xanthan gum,guar-guar, agar-agar, alginates and tyloses, carboxymethyl cellulose andhydroxyethyl cellulose, also relatively high molecular weightpolyethylene glycol monoesters and diesters of fatty acids,polyacrylates (for example Carbopols® [Goodrich] or Synthalens®[Sigma]), polyacrylamides, polyvinyl alcohol and polyvinyl pyrrolidone,surfactants such as, for example, ethoxylated fatty acid glycerides,esters of fatty acids with polyols, for example pentaerythritol ortrimethylol propane, narrow-range fatty alcohol ethoxylates andelectrolytes, such as sodium chloride and ammonium chloride.

Polymers

Suitable cationic polymers are, for example, cationic cellulosederivatives such as, for example, the quaternized hydroxyethyl celluloseobtainable from Amerchol under the name of Polymer JR 400®, cationicstarch, copolymers of diallyl ammonium salts and acrylamides,quaternized vinyl pyrrolidone/vinyl imidazole polymers such as, forexample, Luviquat® (BASF), condensation products of polyglycols andamines, quaternized collagen polypeptides such as, for example,Lauryldimonium Hydroxypropyl Hydrolyzed Collagen (Lamequat® L, Grünau),quaternized wheat polypeptides, polyethyleneimine, cationic siliconepolymers such as, for example, amodimethicone, copolymers of adipic acidand dimethylaminohydroxypropyl diethylenetriamine (Cartaretine®,Sandoz), copolymers of acrylic acid with dimethyl diallyl ammoniumchloride (Merquat® 550, Chemviron), polyaminopolyamides and crosslinkedwater-soluble polymers thereof, cationic chitin derivatives such as, forexample, quaternized chitosan, optionally in microcrystallinedistribution, condensation products of dihaloalkyls, for exampledibromobutane, with bis-dialkylamines, for examplebis-dimethylamino-1,3-propane, cationic guar gum such as, for example,Jaguar® CBS, Jaguar® C-17, Jaguar® C-16 of Celanese, quaternizedammonium salt polymers such as, for example, Mirapol® A-15, Mirapol®AD-1, Mirapol® AZ-1 of Miranol and the various polyquaternium types (forexample 6, 7, 32 or 37) which can be found in the market under thetradenames Rheocare® CC or Ultragel® 300.

Suitable anionic, zwitterionic, amphoteric and nonionic polymers are,for example, vinyl acetate/crotonic acid copolymers, vinylpyrrolidone/vinyl acrylate copolymers, vinyl acetate/butylmaleate/isobornyl acrylate copolymers, methyl vinylether/maleicanhydride copolymers and esters thereof, uncrosslinked andpolyol-crosslinked polyacrylic acids, acrylamidopropyl trimethylammoniumchloride/acrylate copolymers, octylacrylamide/methylmethacrylate/tert.-butylaminoethyl methacrylate/2-hydroxypropylmethacrylate copolymers, polyvinyl pyrrolidone, vinyl pyrrolidone/vinylacetate copolymers, vinyl pyrrolidone/dimethylaminoethylmethacrylate/vinyl caprolactam terpolymers and optionally derivatizedcellulose ethers and silicones.

Pearlizing Waxes

Suitable pearlising waxes are, for example, alkylene glycol esters,especially ethylene glycol distearate; fatty acid alkanolamides,especially cocofatty acid diethanolamide; partial glycerides, especiallystearic acid monoglyceride; esters of polybasic, optionallyhydroxysubstituted carboxylic acids with fatty alcohols containing 6 to22 carbon atoms, especially long-chain esters of tartaric acid; fattycompounds, such as for example fatty alcohols, fatty ketones, fattyaldehydes, fatty ethers and fatty carbonates which contain in all atleast 24 carbon atoms, especially laurone and distearylether; fattyacids, such as stearic acid, hydroxystearic acid or behenic acid, ringopening products of olefin epoxides containing 12 to 22 carbon atomswith fatty alcohols containing 12 to 22 carbon atoms and/or polyolscontaining 2 to 15 carbon atoms and 2 to 10 hydroxyl groups and mixturesthereof.

Silicones

Suitable silicone compounds are, for example, dimethyl polysiloxanes,methylphenyl polysiloxanes, cyclic silicones and amino-, fatty acid-,alcohol-, polyether-, epoxy-, fluorine-, glycoside- and/oralkyl-modified silicone compounds which may be both liquid andresin-like at room temperature. Other suitable silicone compounds aresimethicones which are mixtures of dimethicones with an average chainlength of 200 to 300 dimethylsiloxane units and hydrogenated silicates.A detailed overview of suitable volatile silicones can be found in Toddet al. in Cosm. Toil. 91, 27 (1976).

Waxes and Stabilizers

Besides natural oils used, waxes may also be present in thepreparations, more especially natural waxes such as, for example,candelilla wax, carnauba wax, Japan wax, espartograss wax, cork wax,guaruma wax, rice oil wax, sugar cane wax, ouricury wax, montan wax,beeswax, shellac wax, spermaceti, lanolin (wool wax), uropygial fat,ceresine, ozocerite (earth wax), petrolatum, paraffin waxes andmicrowaxes; chemically modified waxes (hard waxes) such as, for example,montan ester waxes, sasol waxes, hydrogenated jojoba waxes and syntheticwaxes such as, for example, polyalkylene waxes and polyethylene glycolwaxes.

Metal salts of fatty acids such as, for example, magnesium, aluminiumand/or zinc stearate or ricinoleate may be used as stabilizers.

Primary Sun Protection Factors

Primary sun protection factors in the context of the invention are, forexample, organic substances (light filters) which are liquid orcrystalline at room temperature and which are capable of absorbingultraviolet radiation and of releasing the energy absorbed in the formof longer-wave radiation, for example heat.

The formulations according to the invention advantageously contain atleast one UV-A filter and/or at least one UV-B filter and/or a broadbandfilter and/or at least one inorganic pigment. Formulations according tothe invention preferably contain at least one UV-B filter or a broadbandfilter, more particularly preferably at least one UV-A filter and atleast one UV-B filter.

Preferred cosmetic compositions, preferably topical formulationsaccording to the present invention comprise one, two, three or more sunprotection factors selected from the group consisting of 4-aminobenzoicacid and derivatives, salicylic acid derivatives, benzophenonederivatives, dibenzoylmethane derivatives, diphenyl acrylates,3-imidazol-4-yl acrylic acid and esters thereof, benzofuran derivatives,benzylidene malonate derivatives, polymeric UV absorbers containing oneor more organosilicon radicals, cinnamic acid derivatives, camphorderivatives, trianilino-s-triazine derivatives,2-hydroxyphenylbenzotriazole derivatives, phenylbenzimidazole sulfonicacid derivatives and salts thereof, anthranilic acid menthyl esters,benzotriazole derivatives and indole derivatives.

In addition, it is advantageous to combine compounds of formula (I) withactive ingredients which penetrate into the skin and protect the skincells from inside against sunlight-induced damage and reduce the levelof cutaneous matrix metalloproteases. Preferred respective ingredients,so called arylhydrocarbon receptor antagonists, are described in WO2007/128723, incorporated herein by reference. Preferred is2-benzylidene-5,6-dimethoxy-3,3-dimethylindan-1-one.

The UV filters cited below which can be used within the context of thepresent invention are preferred but naturally are not limiting.

UV filters which are preferably used are selected from the groupconsisting of

-   p-aminobenzoic acid-   p-aminobenzoic acid ethyl ester (25 mol) ethoxylated (INCI name:    PEG-25 PABA)-   p-dimethylaminobenzoic acid-2-ethylhexyl ester-   p-aminobenzoic acid ethyl ester (2 mol) N-propoxylated-   p-aminobenzoic acid glycerol ester-   salicylic acid homomenthyl ester (homosalates) (Neo Heliopan® HMS)-   salicylic acid-2-ethylhexyl ester (Neo Heliopan® OS)-   triethanolamine salicylate-   4-isopropyl benzyl salicylate-   anthranilic acid menthyl ester (Neo Heliopan® MA)-   diisopropyl cinnamic acid ethyl ester-   p-methoxycinnamic acid-2-ethylhexyl ester (Neo Heliopan® AV)-   diisopropyl cinnamic acid methyl ester-   p-methoxycinnamic acid isoamyl ester (Neo Heliopan® E 1000)-   p-methoxycinnamic acid diethanolamine salt-   p-methoxycinnamic acid isopropyl ester-   2-phenylbenzimidazole sulfonic acid and salts (Neo Heliopan® Hydro)-   3-(4′-trimethylammonium) benzylidene bornan-2-one methyl sulfate-   beta-imidazole-4(5)-acrylic acid (urocanic acid)-   3-(4′-sulfo)benzylidene bornan-2-one and salts-   3-(4′-methyl benzylidene)-D,L-camphor (Neo Heliopan® MBC)-   3-benzylidene-D,L-camphor-   N-[(2 and 4)-[2-(oxoborn-3-ylidene) methyl]benzyl] acrylamide    polymer-   4,4′-[(6-[4-(1,1-dimethyl)aminocarbonyl)    phenylamino]-1,3,5-triazine-2,4-diyl)diimino]-bis-(benzoic    acid-2-ethylhexyl ester) (Uvasorb® HEB)-   benzylidene malonate polysiloxane (Parsol® SLX)-   glyceryl ethylhexanoate dimethoxycinnamate-   dipropylene glycol salicylate-   tris(2-ethylhexyl)-4,4′,4″-(1,3,5-triazine-2,4,6-triyltriimino)tribenzoate    (=2,4,6-trianilino-(p-carbo-2′-ethylhexyl-1′-oxy)-1,3,5-triazine)    (Uvinul® T150).

Broadband filters which are preferably combined with one or morecompounds of formula (I) in a preparation according to the presentinvention are selected from the group consisting of

-   2-ethylhexyl-2-cyano-3,3-diphenyl acrylate (Neo Heliopan® 303)-   ethyl-2-cyano-3,3′-diphenyl acrylate-   2-hydroxy-4-methoxybenzophenone (Neo Heliopan® BB)-   2-hydroxy-4-methoxybenzophenone-5-sulfonic acid-   dihydroxy-4-methoxybenzophenone-   2,4-dihydroxybenzophenone-   tetrahydroxybenzophenone-   2,2′-dihydroxy-4,4′-dimethoxybenzophenone-   2-hydroxy-4-n-octoxybenzophenone-   2-hydroxy-4-methoxy-4′-methyl benzophenone-   sodium hydroxymethoxybenzophenone sulfonate-   disodium-2,2′-dihydroxy-4,4′-dimethoxy-5,5′-disulfobenzophenone-   phenol,    2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(1,3,3,3-tetramethyl-1-(trimethylsilyl)oxy)disiloxyanyl)    propyl) (Mexoryl® XL)-   2,2′-methylene    bis-(6-(2H-benzotriazol-2-yl)-4-1,1,3,3-tetramethylbutyl) phenol)    (Tinosorb® M)-   2,4-bis-[4-(2-ethylhexyloxy)-2-hydroxyphenyl]-1,3,5-triazine-   2,4-bis-[{(4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine    (Tinosorb® S)-   2,4-bis-[{(4-(3-sulfonato)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine    sodium salt-   2,4-bis-[{(3-(2-propyloxy)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine-   2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-[4-(2-methoxyethyl    carbonyl) phenylamino]-1,3,5-triazine-   2,4-bis-[{4-(3-(2-propyloxy)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-[4-(2-ethylcarboxyl)    phenylamino]-1,3,5-triazine-   2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(1-methylpyrrol-2-yl)-1,3,5-triazine-   2,4-bis-[{4-tris-(trimethylsiloxysilylpropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine-   2,4-bis-[{4-(2″-methylpropenyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine-   2,4-bis-[{4-(1′,1′,1′,3′,5′,5′,5′-heptamethylsiloxy-2″-methylpropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine.

The compositions can comprise further typical detergent and cleansingcomposition ingredients such as UV-A filters filters which arepreferably combined with one or more compounds of formula (I) in apreparation according to the present invention are selected from thegroup consisting of

-   4-isopropyl dibenzoyl methane-   terephthalylidene dibornane sulfonic acid and salts (Mexoryl® SX)-   4-t-butyl-4′-methoxydibenzoyl methane (avobenzone)/(Neo Heliopan®    357)-   phenylene bis-benzimidazyl tetrasulfonic acid disodium salt (Neo    Heliopan® AP)-   2,2′-(1,4-phenylene)-bis-(1H-benzimidazole-4,6-disulfonic acid),    monosodium salt-   2-(4-diethylamino-2-hydroxybenzoyl) benzoic acid hexyl ester    (Uvinul® A Plus)-   indanylidene compounds in accordance with DE 100 55 940 A1 (=WO 2002    038537 A1)

The compositions can comprise further typical detergent and cleansingcomposition ingredients such as UV filters which are more preferablycombined with one or more compounds of formula (I) in a preparationaccording to the present invention are selected from the groupconsisting of

-   p-aminobenzoic acid-   3-(4′-trimethylammonium) benzylidene bornan-2-one methyl sulfate-   salicylic acid homomenthyl ester (Neo Heliopan® HMS)-   2-hydroxy-4-methoxybenzophenone (Neo Heliopan® BB)-   2-phenylbenzimidazole sulfonic acid (Neo Heliopan® Hydro)-   terephthalylidene dibornane sulfonic acid and salts (Mexoryl® SX)-   4-tert-butyl-4′-methoxydibenzoyl methane (Neo Heliopan® 357)-   3-(4′-sulfo)benzylidene bornan-2-one and salts-   2-ethylhexyl-2-cyano-3,3-diphenyl acrylate (Neo Heliopan® 303)-   N-[(2 and 4)-[2-(oxoborn-3-ylidene) methyl]benzyl] acrylamide    polymer-   p-methoxycinnamic acid-2-ethylhexyl ester (Neo Heliopan® AV)-   p-aminobenzoic acid ethyl ester (25 mol) ethoxylated (INCI name:    PEG-25 PABA)-   p-methoxycinnamic acid isoamyl ester (Neo Heliopan® E1000)-   2,4,6-trianilino-(p-carbo-2′-ethylhexyl-1′-oxy)-1,3,5-triazine    (Uvinul® T150)-   phenol,    2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(1,3,3,3-tetramethyl-1-(trimethylsilyl)oxy)disiloxyanyl)-   propyl) (Mexoryl® XL)-   4,4′-[(6-[4-(1,1-dimethyl)aminocarbonyl)    phenylamino]-1,3,5-triazine-2,4-   diyl)diimino]-bis-(benzoic acid-2-ethylhexyl ester) (Uvasorb HEB)-   3-(4′-methyl benzylidene)-D,L-camphor (Neo Heliopan® MBC)-   3-benzylidene camphor-   salicylic acid-2-ethylhexyl ester (Neo Heliopan® OS)-   4-dimethylaminobenzoic acid-2-ethylhexyl ester (Padimate O)-   hydroxy-4-methoxybenzophenone-5-sulfonic acid and Na salt-   2,2′-methylene    bis-(6-(2H-benzotriazol-2-yl)-4-1,1,3,3-tetramethylbutyl) phenol)-   (Tinosorb® M)-   phenylene bis-benzimidazyl tetrasulfonic acid disodium salt (Neo    Heliopan® AP)-   2,4-bis-[{(4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine-   (Tinosorb® S)-   benzylidene malonate polysiloxane (Parsol® SLX)-   menthyl anthranilate (Neo Heliopan® MA)-   2-(4-diethylamino-2-hydroxybenzoyl) benzoic acid hexyl ester    (Uvinul® A Plus)-   indanylidene compounds in accordance with DE 100 55 940 (=WO    02/38537).

Advantageous primary and also secondary sun protection factors arementioned in WO 2005 123101 A1. Advantageously, these preparationscontain at least one UVA filter and/or at least one UVB filter and/or atleast one inorganic pigment. The preparations may be present here invarious forms such as are conventionally used for sun protectionpreparations. Thus, they may be in form of a solution, an emulsion ofthe water-in-oil type (W/O) or of the oil-in-water type (O/W) or amultiple emulsion, for example of the water-in-oil-in-water type(W/O/W), a gel, a hydrodispersion, a solid stick or else an aerosol.

In a further preferred embodiment a formulation according to theinvention contains a total amount of sunscreen agents, i.e. inparticular UV filters and/or inorganic pigments (UV filtering pigments)so that the formulation according to the invention has a lightprotection factor of greater than or equal to 2 (preferably greater thanor equal to 5). Such formulations according to the invention areparticularly suitable for protecting the skin and hair.

Secondary Sun Protection Factors

Besides the groups of primary sun protection factors mentioned above,secondary sun protection factors of the antioxidant type may also beused. Secondary sun protection factors of the antioxidant type interruptthe photochemical reaction chain which is initiated when UV rayspenetrate into the skin. Typical examples are amino acids (for exampleglycine, histidine, tyrosine, tryptophane) and derivatives thereof,imidazoles (for example urocanic acid) and derivatives thereof,peptides, such as D,L-carnosine, D-carnosine, L-carnosine andderivatives thereof (for example anserine), carotinoids, carotenes (forexample alpha-carotene, beta-carotene, lycopene) and derivativesthereof, chlorogenic acid and derivatives thereof, liponic acid andderivatives thereof (for example dihydroliponic acid), aurothioglucose,propylthiouracil and other thiols (for example thioredoxine,glutathione, cysteine, cystine, cystamine and glycosyl, N-acetyl,methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl,alpha-linoleyl, cholesteryl and glyceryl esters thereof) and theirsalts, dilaurylthiodipropionate, distearylthiodipropionate,thiodipropionic acid and derivatives thereof (esters, ethers, peptides,lipids, nucleotides, nucleosides and salts) and sulfoximine compounds(for example butionine sulfoximines, homocysteine sulfoximine, butioninesulfones, penta-, hexa- and hepta-thionine sulfoximine) in very smallcompatible dosages, also (metal) chelators (for examplealpha-hydroxyfatty acids, palmitic acid, phytic acid, lactoferrine),alpha-hydroxy acids (for example citric acid, lactic acid, malic acid),humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTAand derivatives thereof, unsaturated fatty acids and derivatives thereof(for example linoleic acid, oleic acid), folic acid and derivativesthereof, ubiquinone and ubiquinol and derivatives thereof, vitamin C andderivatives thereof (for example ascorbyl palmitate, Mg ascorbylphosphate, ascorbyl acetate), tocopherols and derivatives (for examplevitamin E acetate), vitamin A and derivatives (vitamin A palmitate) andconiferyl benzoate of benzoin resin, rutinic acid and derivativesthereof, glycosyl rutin, ferulic acid, furfurylidene glucitol,carnosine, butyl hydroxytoluene, butyl hydroxyanisole, nordihydroguaiacresin acid, nordihydroguaiaretic acid, trihydroxybutyrophenone, uricacid and derivatives thereof, mannose and derivatives thereof,superoxide dismutase, titanium dioxide (for example dispersions inethanol), zinc and derivatives thereof (for example ZnO, ZnSO₄),selenium and derivatives thereof (for example selenium methionine),stilbenes and derivatives thereof (for example stilbene oxide,trans-stilbene oxide) and derivatives of these active substancessuitable for the purposes of the invention (salts, esters, ethers,sugars, nucleotides, nucleosides, peptides and lipids).

Advantageous inorganic secondary light protection pigments are finelydispersed metal oxides and metal salts which are also mentioned in WO2005 123101 A1. The total quantity of inorganic pigments, in particularhydrophobic inorganic micro-pigments in the finished cosmeticpreparation according to the present invention is advantageously from0.1 to 30% by weight, preferably 0.5 to 10.0% by weight, in each casebased on the total weight of the preparation.

Also preferred are particulate UV filters or inorganic pigments, whichcan optionally be hydrophobed, can be used, such as the oxides oftitanium (TiO₂), zinc (ZnO), iron (Fe₂O₃), zirconium (ZrO₂), silicon(SiO₂), manganese (e.g. MnO), aluminium (Al₂O₃), cerium (e.g. Ce₂O₃)and/or mixtures thereof.

Actives Modulating Skin and/or Hair Pigmentation

Preferred active ingredients for skin and/or hair lightening areselected from the group consisting of: kojic acid(5-hydroxy-2-hydroxymethyl-4-pyranone), kojic acid derivatives,preferably kojic acid dipalmitate, arbutin, ascorbic acid, ascorbic acidderivatives, preferably magnesium ascorbyl phosphate, hydroquinone,hydroquinone derivatives, resorcinol, resorcinol derivatives, preferably4-alkylresorcinols and 4-(1-phenylethyl)1,3-dihydroxybenzene(phenylethyl resorcinol), cyclohexylcarbamates (preferably one or morecyclohexyl carbamates disclosed in WO 2010/122178 and WO 2010/097480),sulfur-containing molecules, preferably glutathione or cysteine,alpha-hydroxy acids (preferably citric acid, lactic acid, malic acid),salts and esters thereof, N-acetyl tyrosine and derivatives, undecenoylphenylalanine, gluconic acid, chromone derivatives, preferably aloesin,flavonoids, 1-aminoethyl phosphinic acid, thiourea derivatives, ellagicacid, nicotinamide (niacinamide), zinc salts, preferably zinc chlorideor zinc gluconate, thujaplicin and derivatives, triterpenes, preferablymaslinic acid, sterols, preferably ergosterol, benzofuranones,preferably senkyunolide, vinyl guiacol, ethyl guiacol, dionic acids,preferably octodecene dionic acid and/or azelaic acid, inhibitors ofnitrogen oxide synthesis, preferably L-nitroarginine and derivativesthereof, 2,7-dinitroindazole or thiocitrulline, metal chelators(preferably alpha-hydroxy fatty acids, phytic acid, humic acid, bileacid, bile extracts, EDTA, EGTA and derivatives thereof), retinoids, soymilk and extract, serine protease inhibitors or lipoic acid or othersynthetic or natural active ingredients for skin and hair lightening,the latter preferably used in the form of an extract from plants,preferably bearberry extract, rice extract, papaya extract, turmericextract, mulberry extract, bengkoang extract, nutgrass extract,liquorice root extract or constituents concentrated or isolatedtherefrom, preferably glabridin or licochalcone A, artocarpus extract,extract of rumex and ramulus species, extracts of pine species (pinus),extracts of vitis species or stilbene derivatives isolated orconcentrated therefrom, saxifrage extract, scutelleria extract, grapeextract and/or microalgae extract, in particular Tetraselmis suecicaExtract.

Preferred skin lighteners as component (b) are kojic acid andphenylethyl resorcinol as tyrosinase inhibitors, beta- andalpha-arbutin, hydroquinone, nicotinamide, dioic acid, Mg ascorbylphosphate and vitamin C and its derivatives, mulberry extract, Bengkoangextract, papaya extract, turmeric extract, nutgrass extract, licoriceextract (containing glycyrrhizin), alpha-hydroxy-acids,4-alkylresorcinols, 4-hydroxyanisole. These skin lighteners arepreferred due to their very good activity, in particular in combinationwith sclareolide according to the present invention. In addition, saidpreferred skin lighteners are readily available.

Advantageous skin and hair tanning active ingredients in this respectare substrates or substrate analogues of tyrosinase such as L-tyrosine,N-acetyl tyrosine, L-DOPA or L-dihydroxyphenylalanine, xanthinealkaloids such as caffeine, theobromine and theophyl-line andderivatives thereof, proopiomelanocortin peptides such as ACTH,alpha-MSH, peptide analogues thereof and other substances which bind tothe melanocortin receptor, peptides such as Val-Gly-Val-Ala-Pro-Gly,Lys-Ile-Gly-Arg-Lys or Leu-Ile-Gly-Lys, purines, pyrimidines, folicacid, copper salts such as copper gluconate, chloride or pyrrolidonate,1,3,4-oxadiazole-2-thiols such as5-pyrazin-2-yl-1,3,4-oxadiazole-2-thiol, curcumin, zinc diglycinate(Zn(Gly)2), manganese(II) bicarbonate complexes (“pseudocat-alases”) asdescribed for example in EP 0 584 178, tetrasubstituted cyclohexenederivatives as described for example in WO 2005/032501, isoprenoids asdescribed in WO 2005/102252 and in WO 2006/010661, melanin derivativessuch as Melasyn-100 and MelanZe, diacyl glycerols, aliphatic or cyclicdiols, psoralens, prostaglandins and analogues thereof, activators ofadenylate cyclase and compounds which activate the transfer ofmelanosomes to keratinocytes such as serine proteases or agonists of thePAR-2 receptor, extracts of plants and plant parts of the chrysanthemumspecies, sanguisorba species, walnut extracts, urucum extracts, rhubarbextracts, microalgae extracts, in particular Isochrysis galbana,trehalose, erythru-lose and dihydroxyacetone. Flavonoids which bringabout skin and hair tinting or browning (e.g. quercetin, rhamnetin,kaempferol, fisetin, genistein, daidzein, chrysin and api-genin,epicatechin, diosmin and diosmetin, morin, quercitrin, naringenin,hesperidin, phloridzin and phloretin) can also be used.

The amount of the aforementioned examples of additional activeingredients for the modulation of skin and hair pigmentation (one ormore compounds) in the products according to the invention is thenpreferably 0.00001 to 30 wt. %, preferably 0.0001 to 20 wt. %,particularly preferably 0.001 to 5 wt. %, based on the total weight ofthe preparation.

Anti-Ageing Actives

In the context of the invention, anti-ageing or biogenic agents are, forexample antioxidants, matrix-metalloproteinase inhibitors (MMPI), skinmoisturizing agents, glycosaminglycan stimulators, anti-inflammatoryagents, TRPV1 antagonists and plant extracts.

Antioxidants. Suitable antioxidants encompass amino acids (preferablyglycine, histidine, tyrosine, tryptophane) and derivatives thereof,imidazoles (preferably urocanic acid) and derivatives thereof, peptides,preferably D,L-carnosine, D-carnosine, L-carnosine and derivativesthereof (preferably anserine), carnitine, creatine, matrikine peptides(preferably lysyl-threonyl-threonyl-lysyl-serine) and palmitoylatedpentapeptides, carotenoids, carotenes (preferably alpha-carotene,beta-carotene, lycopene) and derivatives thereof, lipoic acid andderivatives thereof (preferably dihydrolipoic acid), aurothioglucose,propyl thiouracil and other thiols (preferably thioredoxine,glutathione, cysteine, cystine, cystamine and glycosyl, N-acetyl,methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl,gamma-linoleyl, cholesteryl, glyceryl and oligoglyceryl esters thereof)and salts thereof, dilauryl thiodipropionate, distearylthiodipropionate, thiodipropionic acid and derivatives thereof(preferably esters, ethers, peptides, lipids, nucleotides, nucleosidesand salts) and sulfoximine compounds (preferably buthioninesulfoximines, homocysteine sulfoximine, buthionine sulfones, penta-,hexa-, heptathionine sulfoximine) in very small tolerated doses (e.g.pmol to μmol/kg), also (metal) chelators (preferably alpha-hydroxy fattyacids, palmitic acid, phytic acid, lactoferrin, alpha-hydroxy acids(preferably citric acid, lactic acid, malic acid), humic acid, bileacid, bile extracts, tannins, bilirubin, biliverdin, EDTA, EGTA andderivatives thereof), unsaturated fatty acids and derivatives thereof(preferably gamma-linolenic acid, linoleic acid, oleic acid), folic acidand derivatives thereof, ubiquinone and derivatives thereof, ubiquinoland derivatives thereof, vitamin C and derivatives (preferably ascorbylpalmitate, Mg ascorbyl phosphate, ascorbyl acetate, ascorbyl glucoside),tocopherols and derivatives (preferably vitamin E acetate), vitamin Aand derivatives (vitamin A palmitate) and coniferyl benzoate of benzoicresin, rutinic acid and derivatives thereof, flavonoids and glycosylatedprecursors thereof, in particular quercetin and derivatives thereof,preferably alpha-glucosyl rutin, rosmarinic acid, carnosol, carnosolicacid, resveratrol, caffeic acid and derivatives thereof, sinapic acidand derivatives thereof, ferulic acid and derivatives thereof,curcuminoids, chlorogenic acid and derivatives thereof, retinoids,preferably retinyl palmitate, retinol or tretinoin, ursolic acid,levulinic acid, butyl hydroxytoluene, butyl hydroxyanisole,nordihydroguaiac acid, nordihydroguaiaretic acid,trihydroxybutyrophenone, uric acid and derivatives thereof, mannose andderivatives thereof, zinc and derivatives thereof (preferably ZnO,ZnSO₄), selenium and derivatives thereof (preferably seleniummethionine), superoxide dismutase, stilbenes and derivatives thereof(preferably stilbene oxide, trans-stilbene oxide) and the derivatives(salts, esters, ethers, sugars, nucleotides, nucleosides, peptides andlipids) of these cited active ingredients which are suitable accordingto the invention or extracts or fractions of plants having anantioxidant effect, preferably green tea, rooibos, honeybush, grape,rosemary, sage, melissa, thyme, lavender, olive, oats, cocoa, ginkgo,ginseng, liquorice, honeysuckle, sophora, pueraria, pinus, citrus,Phyllanthus emblica or St. John's wort, grape seeds, wheat germ,Phyllanthus emblica, coenzymes, preferably coenzyme Q10, plastoquinoneand menaquinone. Preferred antioxidants are selected from the groupconsisting of vitamin A and derivatives, vitamin C and derivatives,tocopherol and derivatives, preferably tocopheryl acetate, andubiquinone.

If vitamin E and/or derivatives thereof are used as the antioxidant(s),it is advantageous to choose their concentrations from the range fromabout 0.001 to about 10% b.w. based on the total weight of theformulation. If vitamin A or vitamin A derivatives or carotenes orderivatives thereof are used as the antioxidant(s), it is advantageousto choose their concentrations from the range from about 0.001 to about10% b.w. based on the total weight of the formulation.

Matrix-Metalloproteinase inhibitors (MMPI). Preferred compositionscomprise matrix-metalloproteinase inhibitors, especially thoseinhibiting matrix-metalloproteinases enzymatically cleaving collagen,selected from the group consisting of: ursolic acid, retinyl palmitate,propyl gallate, precocenes,6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)benzopyran,3,4-dihydro-6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)-benzopyran,benzamidine hydrochloride, the cysteine proteinase inhibitorsN-ethylmalemide and epsilon-amino-n-caproic acid of the serinproteaseinhibitors: phenylmethylsufonylfluoride, collhibin (company Pentapharm;INCI: hydrolysed rice protein), oenotherol (company Soliance; INCI:propylene glycol, aqua, Oenothera biennis root extract, ellagic acid andellagitannins, for example from pomegranate), phosphoramidonehinokitiol, EDTA, galardin, EquiStat (company Collaborative Group; applefruit extract, soya seed extract, ursolic acid, soya isoflavones andsoya proteins), sage extracts, MDI (company Atrium; INCI:glycosaminoglycans), fermiskin (company Silab/Mawi; INCI: water andlentinus edodes extract), actimp 1.9.3 (company Expanscience/Rahn; INCI:hydrolysed lupine protein), lipobelle soyaglycone (company Mibelle;INCI: alcohol, polysorbate 80, lecithin and soy isoflavones), extractsfrom green and black tea and further plant extracts, which are listed inWO 02 069992 A1 (see tables 1-12 there, incorporated herein byreference), proteins or glycoproteins from soya, hydrolysed proteinsfrom rice, pea or lupine, plant extracts which inhibit MMPs, preferablyextracts from shitake mushrooms, extracts from the leaves of theRosaceae family, sub-family Rosoideae, quite particularly extracts ofblackberry leaf (preferably as described in WO 2005 123101 A1,incorporated herein by reference) as e.g. SymMatrix (company Symrise,INCI: Maltodextrin, Rubus Fruticosus (Blackberry) Leaf Extract).Preferred actives of are selected from the group consisting of retinylpalmitate, ursolic acid, extracts from the leaves of the Rosaceaefamily, sub-family Rosoideae, genistein and daidzein.

Skin-moisturizing agents. Preferred skin moisturizing agents areselected from the group consisting of alkane diols or alkane triolscomprising 3 to 12 carbon atoms, preferably C₃-C₁₀-alkane diols andC₃-C₁₀-alkane triols. More preferably the skin moisturizing agents areselected from the group consisting of: glycerol, 1,2-propylene glycol,1,2-butylene glycol, 1,3-butylene glycol, 1,2-pentanediol,1,2-hexanediol, 1,2-octanediol and 1,2-decanediol.

Glycosaminoglycan stimulators. Preferred compositions comprisesubstances stimulating the synthesis of glycosaminoglycans selected fromthe group consisting of hyaluronic acid and derivatives or salts,Subliskin (Sederma, INCI: Sinorhizobium Meliloti Ferment Filtrate, CetylHydroxyethylcellulose, Lecithin), Hyalufix (BASF, INCI: Water, ButyleneGlycol, Alpinia galanga leaf extract, Xanthan Gum, Caprylic/CapricTriglyceride), Stimulhyal (Soliance, INCI: Calcium ketogluconate),Syn-Glycan (DSM, INCI: Tetradecyl Aminobutyroylvalyl-aminobutyric UreaTrifluoroacetate, Glycerin, Magnesium chloride), Kalpariane (BiotechMarine), DC Upregulex (Distinctive Cosmetic Ingredients, INCI: Water,Butylene Glycol, Phospholipids, Hydrolyzed Sericin), glucosamine,N-acetyl glucosamine, retinoids, preferably retinol and vitamin A,Arctium lappa fruit extract, Eriobotrya japonica extract, Genkwanin,N-Methyl-L-serine, (−)-alpha-bisabolol or synthetic alpha-bisabolol suchas e.g. Dragosantol and Dragosantol 100 from Symrise, oat glucan,Echinacea purpurea extract and soy protein hydrolysate. Preferredactives are selected from the group consisting of hyaluronic acid andderivatives or salts, retinol and derivatives, (−)-alpha-bisabolol orsynthetic alpha-bisabolol such as e.g. Dragosantol and Dragosantol 100from Symrise, oat glucan, Echinacea purpurea extract, SinorhizobiumMeliloti Ferment Filtrate, Calcium ketogluconate, Alpinia galanga leafextract and tetradecyl aminobutyroylvalylaminobutyric ureatrifluoroacetate.

Anti-inflammatory agents. The compositions may also containanti-inflammatory and/or redness and/or itch ameliorating ingredients,in particular steroidal substances of the corticosteroid type selectedfrom the group consisting of hydrocortisone, dexamethasone,dexamethasone phosphate, methyl prednisolone or cortisone, areadvantageously used as anti-inflammatory active ingredients or activeingredients to relieve reddening and itching, the list of which can beextended by the addition of other steroidal anti-inflammatories.Non-steroidal anti-inflammatories can also be used. Examples which canbe cited here are oxicams such as piroxicam or tenoxicam; salicylatessuch as aspirin, disalcid, solprin or fendosal; acetic acid derivativessuch as diclofenac, fenclofenac, indomethacin, sulindac, tolmetin orclindanac; fenamates such as mefenamic, meclofenamic, flufenamic orniflumic; propionic acid derivatives such as ibuprofen, naproxen,benoxaprofen or pyrazoles such as phenylbutazone, oxyphenylbutazone,febrazone or azapropazone. Anthranilic acid derivatives, in particularavenanthramides described in WO 2004 047833 A1, are preferred anti-itchingredients in a composition according to the present invention.

Also useful are natural or naturally occurring anti-inflammatorymixtures of substances or mixtures of substances that alleviatereddening and/or itching, in particular extracts or fractions fromcamomile, Aloe vera, Commiphora species, Rubia species, willow,willow-herb, oats, calendula, arnica, St John's wort, honeysuckle,rosemary, Passiflora incarnata, witch hazel, ginger or Echinacea;preferably selected from the group consisting of extracts or fractionsfrom camomile, Aloe vera, oats, calendula, arnica, honeysuckle,rosemary, witch hazel, ginger or Echinacea, and/or pure substances,preferably alpha-bisabolol, apigenin, apigenin-7-glucoside, gingerols,shogaols, gingerdiols, dehydrogingerdiones, paradols, natural ornaturally occuring avenanthramides, preferably tranilast, avenanthramideA, avenanthramide B, avenanthramide C, non-natural or non-naturallyoccuring avenanthramides, preferably dihydroavenanthramide D,dihydroavenanthramide E, avenanthramide D, avenan-thramide E,avenanthramide F, boswellic acid, phytosterols, glycyrrhizin, glabridinand licochalcone A; preferably selected from the group consisting ofalphabisabolol, natural avenanthramides, non-natural avenanthramides,preferably dihydroavenanthramide D (as described in WO 2004 047833 A1),boswellic acid, phytosterols, glycyrrhizin, and licochalcone A, and/orallantoin, panthenol, lanolin, (pseudo-)ceramides [preferably Ceramide2, hydroxypropyl bispalmitamide MEA, cetyloxypropyl glycerylmethoxypropyl myristamide, N-(1-hexadecanoyl)-4-hydroxy-L-proline(1-hexadecyl) ester, hydroxyethyl palmityl oxyhydroxypropylpalmitamide], glycosphingolipids, phytosterols, chitosan, mannose,lactose and β-glucans, in particular 1,3-1,4-β-glucan from oats.

When bisabolol is used in the context of the present invention it can beof natural or synthetic origin, and is preferably “alpha-bisabolol”.Preferably, the bisabolol used is synthetically prepared or natural(−)-alpha-bisabolol and/or synthetic mixed-isomer alpha-bisabolol. Ifnatural (−)-alpha-bisabolol is used, this can also be employed as aconstituent of an essential oil or of a plant extract or of a fractionthereof, for example as a constituent of (fractions of) oil or extractsof camomile or of Vanillosmopsis (in particular Vanillosmopsiserythropappa or Vanillosmopsis arborea). Synthetic alpha-bisabolol isobtainable, for example, under the name “Dragosantol” from Symrise.

In case ginger extract is used in the context of the present invention,preferably extracts of the fresh or dried ginger root are used which areprepared by extraction with methanol, ethanol, iso-propanol, acetone,ethyl acetate, carbon dioxide (CO2), hexane, methylene chloride,chloroform or other solvents or solvent mixtures of comparable polarity.The extracts are characterized by the presence of active skinirritation-reducing amounts of constituents such as e.g. gingerols,shogaols, gingerdiols, dehydrogingerdiones and/or paradols.

TRPV1 antagonists. Suitable compounds which reduce the hypersensitivityof skin nerves based on their action as TRPV1 antagonists, encompasse.g. trans-4-tert-butyl cyclohexanol as described in WO 2009 087242 A1,or indirect modulators of TRPV1 by an activation of the μ-receptor, e.g.acetyl tetrapeptide-15, are preferred.

Desquamating agents. The compositions may also contain desquamatingagents (component b5) in amounts of about 0.1 to about 30% b.w.preferably about 0.5 to about 15% b.w., particularly preferably about 1to about 10% b.w. based on the total weight of the preparation. Theexpression “desquamating agent” is understood to mean any compoundcapable of acting:

-   -   either directly on desquamation by promoting exfoliation, such        as β-hydroxy acids, in particular salicylic acid and its        derivatives (including 5-n-octanoylsalicylic acid); α-hydroxy        acids, such as glycolic, citric, lactic, tartaric, malic or        mandelic acids; urea; gentisic acid; oligofucoses; cinnamic        acid; extract of Sophora japonica; resveratrol and some        derivatives of jasmonic acid;    -   or on the enzymes involved in the desquamation or the        degradation of the corneodesmosomes, glycosidases, stratum        corneum chymotryptic enzyme (SCCE) or other proteases (trypsin,        chymotrypsin-like). There may be mentioned agents chelating        inorganic salts: EDTA; N-acyl-N,N′,N′-ethylenediaminetriacetic        acid; aminosulphonic compounds and in particular        (N-2-hydroxyethylpiperazine-N-2-ethane)sulphonic acid (HEPES);        derivatives of 2-oxothiazolidine-4-carboxylic acid        (procysteine); derivatives of alpha-amino acids of the glycine        type (as described in EP-0 852 949, and sodium methylglycine        diacetate marketed by BASF under the trade name TRILON M);        honey; sugar derivatives such as O-octanoyl-6-D-maltose and        N-acetylglucosamine; chestnut extracts such as those marketed by        the company SILAB under the name Recoverine®, prickly pear        extracts such as those marketed under the name Exfolactive® by        the company SILAB, or Phytosphingosine SLC® (phytosphingosine        grafted with a salicylic acid) marketed by the company Degussa.

Desquamating agents suitable for the invention may be chosen inparticular from the group comprising sulphonic acids, calcium chelators,α-hydroxy acids such as glycolic, citric, lactic, tartaric, malic ormandelic acids; ascorbic acid and its derivatives such as ascorbylglucoside and magnesium ascorbyl phosphate; nicotinamide; urea;(N-2-hydroxyethylpiperazine-N-2-ethane)sulphonic acid (HEPES), β-hydroxyacids such as salicylic acid and its derivatives, retinoids such asretinol and its esters, retinal, retinoic acid and its derivatives,those described in the documents FR 2570377 A1, EP 0199636 A1, EP0325540 A1, EP 0402072 A1, chestnut or prickly pear extracts, inparticular marketed by SILAB; reducing compounds such as cysteine orcysteine precursors.

Desquamating agents which can be used are also nicotinic acid and itsesters and nicotinamide, also called vitamin B3 or vitamin PP, andascorbic acid and its precursors, as described in particular inapplication EP 1529522 A1.

Anti-cellulite agents. Anti-cellulite agents and lipolytic agents arepreferably selected from the group consisting of those described in WO2007/077541, and beta-adrenergic receptor agonists such as synephrineand its derivatives, and cyclohexyl carbamates described in WO2010/097479. Agents enhancing or boosting the activity of anti-celluliteagents, in particular agents which stimulate and/or depolarise C nervefibres, are preferably selected from the group consisting of capsaicinand derivatives thereof, vanillyl-nonylamid and derivatives thereof,L-carnitine, coenzyme A, isoflavonoides, soy extracts, ananas extractand conjugated linoleic acid.

Fat enhancing agents. Formulations and products according to the presentinvention may also comprise one or more fat enhancing and/or adipogenicagents as well as agents enhancing or boosting the activity of fatenhancing agents. A fat enhancing agent is for examplehydroxymethoxyphenyl propylmethylmethoxybenzofuran (trade name: Sym3D®).

Hair Growth Activators or Inhibitors

Formulations and products according to the present invention may alsocomprise one or more hair growth activators, i.e. agents to stimulatehair growth. Hair growth activators are preferably selected from thegroup consisting of pyrimidine derivatives such as2,4-diaminopyrimidine-3-oxide (Aminexil),2,4-diamino-6-piperidinopyrimidine-3-oxide (Minoxidil) and derivativesthereof, 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidineand its derivatives, xanthine alkaloids such as caffeine, theobromineand theophylline and derivatives thereof, quercetin and derivatives,dihydroquercetin (taxifolin) and derivatives, potassium channel openers,antiandrogenic agents, synthetic or natural 5-reductase inhibitors,nicotinic acid esters such as tocopheryl nicotinate, benzyl nicotinateand C1-C6 alkyl nicotinate, proteins such as for example the tripeptideLys-Pro-Val, diphencypren, hormons, finasteride, dutasteride, flutamide,bicalutamide, pregnane derivatives, progesterone and its derivatives,cyproterone acetate, spironolactone and other diuretics, calcineurininhibitors such as FK506 (Tacrolimus, Fujimycin) and its derivatives,Cyclosporin A and derivatives thereof, zinc and zinc salts, polyphenols,procyanidins, proanthocyanidins, phytosterols such as for examplebeta-sitosterol, biotin, eugenol, (±)-beta-citronellol, panthenol,glycogen for example from mussels, extracts from microorganisms, algae,plants and plant parts of for example the genera dandelion (Leontodon orTaraxacum), Orthosiphon, Vitex, Coffea, Paullinia, Theobroma, Asiasarum,Cucurbita or Styphnolobium, Serenoa repens (saw palmetto), Sophoraflavescens, Pygeum africanum, Panicum miliaceum, Cimicifuga racemosa,Glycine max, Eugenia caryophyllata, Cotinus coggygria, Hibiscusrosa-sinensis, Camellia sinensis, Ilex paraguariensis, Isochrysisgalbana, licorice, grape, apple, barley or hops or/and hydrolysates fromrice or wheat.

Alternatively, formulations and products according to the presentinvention may comprise one or more hair growth inhibitors (as describedabove), i.e. agents to reduce or prevent hair growth. Hair growthinhibitors are preferably selected from the group consisting of activin,activin derivatives or activin agonists, ornithine decarboxylaseinhibitors such as alpha-difluoromethylornithine or pentacyclictriterpenes like for example ursolic acid, betulin, betulinic acid,oleanolic acid and derivatives thereof, 5alpha-reductase inhibitors,androgen receptor antagonists, S-adenosylmethionine decarboxylaseinhibitors, gamma-glutamyl transpeptidase inhibitors, transglutaminaseinhibitors, soybean-derived serine protease inhibitors, extracts frommicroorganisms, algae, different microalgae or plants and plant parts offor example the families Leguminosae, Solanaceae, Graminae,Asclepiadaceae or Cucurbitaceae, the genera Chondrus, Gloiopeltis,Ceramium, Durvillea, Glycine max, Sanguisorba officinalis, Calendulaofficinalis, Hamamelis virginiana, Arnica montana, Salix alba, Hypericumperforatum or Gymnema sylvestre.

Cooling Agents

The compositions may also contain one or more substances with aphysiological cooling effect (cooling agents), which are preferablyselected here from the following list: menthol and menthol derivatives(for example L-menthol, D-menthol, racemic menthol, isomenthol,neoisomenthol, neomenthol) menthylethers (for example(I-menthoxy)-1,2-propandiol, (I-menthoxy)-2-methyl-1,2-propandiol,I-menthyl-methylether), menthylesters (for example menthylformiate,menthylacetate, menthylisobutyrate, menthyllactates,L-menthyl-L-lactate, L-menthyl-D-lactate, menthyl-(2-methoxy)acetate,menthyl-(2-methoxyethoxy)acetate, menthylpyroglutamate),menthylcarbonates (for example menthylpropyleneglycolcarbonate,menthylethyleneglycolcarbonate, menthylglycerolcarbonate or mixturesthereof), the semi-esters of menthols with a dicarboxylic acid orderivatives thereof (for example mono-menthylsuccinate,mono-menthylglutarate, mono-menthylmalonate, O-menthyl succinic acidester-N,N-(dimethyl)amide, O-menthyl succinic acid ester amide),menthanecarboxylic acid amides (in this case preferablymenthanecarboxylic acid-N-ethylamide [WS3] orN^(α)-(menthanecarbonyl)glycinethylester [WS5], as described in U.S.Pat. No. 4,150,052, menthanecarboxylic acid-N-(4-cyanophenyl)amide ormenthanecarboxylic acid-N-(4-cyanomethylphenyl)amide as described in WO2005 049553 A1, methanecarboxylic acid-N-(alkoxyalkyl)amides), menthoneand menthone derivatives (for example L-menthone glycerol ketal),2,3-dimethyl-2-(2-propyl)-butyric acid derivatives (for example2,3-dimethyl-2-(2-propyl)-butyric acid-N-methylamide [WS23]), isopulegolor its esters (I-(−)-isopulegol, I-(−)-isopulegolacetate), menthanederivatives (for example p-menthane-3,8-diol), cubebol or synthetic ornatural mixtures, containing cubebol, pyrrolidone derivatives ofcycloalkyldione derivatives (for example3-methyl-2(1-pyrrolidinyl)-2-cyclopentene-1-one) ortetrahydropyrimidine-2-one (for example iciline or related compounds, asdescribed in WO 2004/026840), further carboxamides (for exampleN-(2-(pyridin-2-yl)ethyl)-3-p-menthanecarboxamide or related compounds),(1R,2S,5R)-N-(4-Methoxyphenyl)-5-methyl-2-(1-isopropyl)cyclohexane-carboxamide[WS12], oxamates (preferably those described in EP 2033688 A2).

Anti-Microbial Agents

Suitable anti-microbial agents are, in principle, all substanceseffective against Gram-positive bacteria, such as, for example,4-hydroxybenzoic acid and its salts and esters,N-(4-chlorophenyl)-N′-(3,4-dichlorophenyl)urea,2,4,4′-trichloro-2′-hydroxy-diphenyl ether (triclosan),4-chloro-3,5-dimethyl-phenol, 2,2′-methylenebis(6-bromo-4-chlorophenol),3-methyl-4-(1-methylethyl)phenol, 2-benzyl-4-chloro-phenol,3-(4-chlorophenoxy)-1,2-propanediol, 3-iodo-2-propynyl butylcarbamate,chlorhexidine, 3,4,4′-trichlorocarbanilide (TTC), antibacterialfragrances, thymol, thyme oil, eugenol, oil of cloves, menthol, mintoil, farnesol, phenoxyethanol, glycerol monocaprate, glycerolmonocaprylate, glycerol monolaurate (GML), diglycerol monocaprate (DMC),salicylic acid N-alkylamides, such as, for example, n-octylsalicylamideor n-decylsalicylamide.

Enzyme Inhibitors

Suitable enzyme inhibitors are, for example, esterase inhibitors. Theseare preferably trialkyl citrates, such as trimethyl citrate, tripropylcitrate, triisopropyl citrate, tributyl citrate and, in particular,triethyl citrate (Hydagen CAT). The substances inhibit enzyme activity,thereby reducing the formation of odour. Other substances which aresuitable esterase inhibitors are sterol sulfates or phosphates, such as,for example, lanosterol, cholesterol, campesterol, stigmasterol andsitosterol sulfate or phosphate, dicarboxylic acids and esters thereof,such as, for example, glutaric acid, monoethyl glutarate, diethylglutarate, adipic acid, monoethyl adipate, diethyl adipate, malonic acidand diethyl malonate, hydroxycarboxylic acids and esters thereof, suchas, for example, citric acid, malic acid, tartaric acid or diethyltartrate, and zinc glycinate.

Odour Absorbers and Antiperspirant Active Agents

Suitable odour absorbers are substances which are able to absorb andlargely retain odour-forming compounds. They lower the partial pressureof the individual components, thus also reducing their rate ofdiffusion. It is important that perfumes must remain unimpaired in thisprocess. Odour absorbers are not effective against bacteria. Theycomprise, for example, as main constituent, a complex zinc salt ofricinoleic acid or specific, largely odour-neutral fragrances which areknown to the person skilled in the art as “fixatives”, such as, forexample, extracts of labdanum or styrax or certain abietic acidderivatives. The odour masking agents are fragrances or perfume oils,which, in addition to their function as odour masking agents, give thedeodorants their respective fragrance note. Perfume oils which may bementioned are, for example, mixtures of natural and syntheticfragrances. Natural fragrances are extracts from flowers, stems andleaves, fruits, fruit peels, roots, woods, herbs and grasses, needlesand branches, and resins and balsams. Also suitable are animal products,such as, for example, civet and castoreum. Typical synthetic fragrancecompounds are products of the ester, ether, aldehyde, ketone, alcohol,and hydrocarbon type. Fragrance compounds of the ester type are, forexample, benzyl acetate, p-tert-butylcyclohexyl acetate, linalylacetate, phenylethyl acetate, linalyl benzoate, benzyl formate, allylcyclohexylpropionate, styrallyl propionate and benzyl salicylate. Theethers include, for example, benzyl ethyl ether, and the aldehydesinclude, for example, the linear alkanals having 8 to 18 carbon atoms,citral, citronellal, citronellyloxyacetaldehyde, cyclamen aldehyde,hydroxycitronellal, lilial and bourgeonal, the ketones include, forexample, the ionones and methyl cedryl ketone, the alcohols includeanethole, citronellol, eugenol, isoeugenol, geraniol, linaool,phenylethyl alcohol and terpineol, and the hydrocarbons include mainlythe terpenes and balsams. Preference is, however, given to usingmixtures of different fragrances which together produce a pleasingfragrance note. Essential oils of relatively low volatility, which aremostly used as aroma components, are also suitable as perfume oils, e.g.sage oil, camomile oil, oil of cloves, melissa oil, mint oil, cinnamonleaf oil, linden flower oil, juniper berry oil, vetiver oil, olibanumoil, galbanum oil, labdanum oil and lavandin oil. Preference is given tousing bergamot oil, dihydromyrcenol, lilial, lyral, citronellol,phenylethyl alcohol, α-hexylcinnamaldehyde, geraniol, benzylacetone,cyclamen aldehyde, linalool, boisambrene forte, ambroxan, indole,hedione, sandelice, lemon oil, mandarin oil, orange oil, allyl amylglycolate, cyclovertal, lavandin oil, clary sage oil, β-damascone,geranium oil bourbon, cyclohexyl salicylate, Vertofix coeur,iso-E-super, Fixolide NP, evernyl, iraldein gamma, phenylacetic acid,geranyl acetate, benzyl acetate, rose oxide, romilat, irotyl andfloramat alone or in mixtures.

Suitable astringent antiperspirant active ingredients are primarilysalts of aluminium, zirconium or of zinc. Such suitable antihydroticactive ingredients are, for example, aluminium chloride, aluminiumchlorohydrate, aluminium dichlorohydrate, aluminium sesquichlorohydrateand complex compounds thereof, e.g. with 1,2-propylene glycol, aluminiumhydroxyallantoinate, aluminium chloride tartrate, aluminium zirconiumtrichlorohydrate, aluminium zirconium tetrachlorohydrate, aluminiumzirconium pentachlorohydrate and complex compounds thereof, e.g. withamino acids, such as glycine.

Film Formers and Anti-Dandruff Agents

Standard film formers are, for example, chitosan, microcrystallinechitosan, quaternized chitosan, polyvinyl pyrrolidone, vinylpyrrolidone/vinyl acetate copolymers, polymers of the acrylic acidseries, quaternary cellulose derivatives, collagen, hyaluronic acid andsalts thereof and similar compounds.

Suitable antidandruff agents are Pirocton Olamin(1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2-(1H)-pyridinonemonoethanolamine salt), Baypival® (Climbazole), Ketoconazol®(4-acetyl-1-{4-[2-(2,4-dichlorophenyl)r-2-(1H-imidazol-1-ylmethyl)-1,3-dioxylan-c-4-ylmethoxyphenyl}-piperazine,ketoconazole, elubiol, selenium disulfide, colloidal sulfur, sulfurpolyethylene glycol sorbitan monooleate, sulfur ricinol polyethoxylate,sulfur tar distillate, salicylic acid (or in combination withhexachlorophene), undecylenic acid, monoethanolamide sulfosuccinate Nasalt, Lamepon® UD (protein/undecylenic acid condensate), zincpyrithione, aluminium pyrithione and magnesium pyrithione/dipyrithionemagnesium sulfate.

Carriers and Hydrotropes

Preferred cosmetics carrier materials are solid or liquid at 25° C. and1013 mbar (including highly viscous substances) as for example glycerol,1,2-propylene glycol, 1,2-butylene glycol, 1,3-propylene glycol,1,3-butylene glycol, ethanol, water and mixtures of two or more of saidliquid carrier materials with water. Optionally, these preparationsaccording to the invention may be produced using preservatives orsolubilizers. Other preferred liquid carrier substances, which may be acomponent of a preparation according to the invention are selected fromthe group consisting of oils such as vegetable oil, neutral oil andmineral oil.

Preferred solid carrier materials, which may be a component of apreparation according to the invention are hydrocolloids, such asstarches, degraded starches, chemically or physically modified starches,dextrins, (powdery) maltodextrins (preferably with a dextrose equivalentvalue of 5 to 25, preferably of 10-20), lactose, silicon dioxide,glucose, modified celluloses, gum arabic, ghatti gum, traganth, karaya,carrageenan, pullulan, curdlan, xanthan gum, gellan gum, guar flour,carob bean flour, alginates, agar, pectin and inulin and mixtures of twoor more of these solids, in particular maltodextrins (preferably with adextrose equivalent value of 15-20), lactose, silicon dioxide and/orglucose.

In addition, hydrotropes, for example ethanol, isopropyl alcohol orpolyols, may be used to improve flow behaviour. Suitable polyolspreferably contain 2 to 15 carbon atoms and at least two hydroxylgroups. The polyols may contain other functional groups, more especiallyamino groups, or may be modified with nitrogen. Typical examples are

-   -   glycerol;    -   alkylene glycols such as, for example, ethylene glycol,        diethylene glycol, propylene glycol, butylene glycol, hexylene        glycol and polyethylene glycols with an average molecular weight        of 100 to 1000 Dalton;    -   technical oligoglycerol mixtures with a degree of        self-condensation of 1.5 to 10, such as for example technical        diglycerol mixtures with a diglycerol content of 40 to 50% by        weight;    -   methylol compounds such as, in particular, trimethylol ethane,        trimethylol propane, trimethylol butane, pentaerythritol and        dipentaerythritol;    -   lower alkyl glucosides, particularly those containing 1 to 8        carbon atoms in the alkyl group, for example methyl and butyl        glucoside;    -   sugar alcohols containing 5 to 12 carbon atoms, for example        sorbitol or mannitol,    -   sugars containing 5 to 12 carbon atoms, for example glucose or        sucrose;    -   amino sugars, for example glucamine;    -   dialcoholamines, such as diethanolamine or        2-aminopropane-1,3-diol.

Preservatives

Suitable preservatives are, for example, phenoxyethanol, formaldehydesolution, parabens, pentanediol or sorbic acid and the other classes ofcompounds listed in Appendix 6, Parts A and B of the Kosmetikverordnung(“Cosmetics Directive”).

Perfume Oils and Fragrances

Suitable perfume oils are mixtures of natural and synthetic perfumes.Natural perfumes include the extracts of blossoms (lily, lavender, rose,jasmine, neroli, ylang-ylang), stems and leaves (geranium, patchouli,petitgrain), fruits (anise, coriander, caraway, juniper), fruit peel(bergamot, lemon, orange), roots (nutmeg, angelica, celery, cardamom,costus, iris, calmus), woods (pinewood, sandalwood, guaiac wood,cedarwood, rosewood), herbs and grasses (tarragon, lemon grass, sage,thyme), needles and branches (spruce, fir, pine, dwarf pine), resins andbalsams (galbanum, elemi, benzoin, myrrh, olibanum, opoponax). Animalraw materials, for example civet and beaver, may also be used. Typicalsynthetic perfume compounds are products of the ester, ether, aldehyde,ketone, alcohol and hydrocarbon type. Examples of perfume compounds ofthe ester type are benzyl acetate, phenoxyethyl isobutyrate,p-tert.butyl cyclohexylacetate, linalyl acetate, dimethyl benzylcarbinyl acetate, phenyl ethyl acetate, linalyl benzoate, benzylformate, ethylmethyl phenyl glycinate, allyl cyclohexyl propionate,styrallyl propionate and benzyl salicylate. Ethers include, for example,benzyl ethyl ether while aldehydes include, for example, the linearalkanals containing 8 to 18 carbon atoms, citral, citronellal,citronellyloxyacetaldehyde, cyclamen aldehyde, hydroxycitronellal,lilial and bourgeonal. Examples of suitable ketones are the ionones,▪-isomethylionone and methyl cedryl ketone. Suitable alcohols areanethol, citronellol, eugenol, isoeugenol, geraniol, linalool,phenylethyl alcohol and terpineol. The hydrocarbons mainly include theterpenes and balsams. However, it is preferred to use mixtures ofdifferent perfume compounds which, together, produce an agreeableperfume. Other suitable perfume oils are essential oils of relativelylow volatility which are mostly used as aroma components. Examples aresage oil, camomile oil, clove oil, melissa oil, mint oil, cinnamon leafoil, lime-blossom oil, juniper berry oil, vetiver oil, olibanum oil,galbanum oil, ladanum oil and lavendin oil. The following are preferablyused either individually or in the form of mixtures: bergamot oil,dihydromyrcenol, lilial, lyral, citronellol, phenylethyl alcohol,hexylcinnamaldehyde, geraniol, benzyl acetone, cyclamen aldehyde,linalool, Boisambrene Forte, Ambroxan, indole, hedione, sandelice,citrus oil, mandarin oil, orange oil, allylamyl glycolate, cyclovertal,lavendin oil, clary oil, damascone, geranium oil bourbon, cyclohexylsalicylate, Vertofix Coeur, Iso-E-Super, Fixolide NP, evernyl, iraldeingamma, phenylacetic acid, geranyl acetate, benzyl acetate, rose oxide,romillat, irotyl and floramat.

Dyes

Suitable dyes are any of the substances suitable and approved forcosmetic purposes as listed, for example, in the publication“Kosmetische Färbemittel” of the Farbstoffkommission der DeutschenForschungsgemeinschaft, Verlag Chemie, Weinheim, 1984, pages 81 to 106.Examples include cochineal red A (C.I. 16255), patent blue V (C.I.42051), indigotin (C.I. 73015), chlorophyllin (C.I. 75810), quinolineyellow (C.I. 47005), titanium dioxide (C.I. 77891), indanthrene blue RS(C.I. 69800) and madder lake (C.I. 58000). Luminol may also be presentas a luminescent dye. Advantageous coloured pigments are for exampletitanium dioxide, mica, iron oxides (e.g. Fe₂O₃ Fe₃O₄, FeO(OH)) and/ortin oxide. Advantageous dyes are for example carmine, Berlin blue,chromium oxide green, ultramarine blue and/or manganese violet.

Preparations

Preferred compositions according to the present inventions are selectedfrom the group of products for treatment, protecting, care and cleansingof the skin and/or hair or as a make-up product, preferably as aleave-on product (meaning that the one or more compounds of formula (I)stay on the skin and/or hair for a longer period of time, compared torinse-off products, so that the moisturizing and/or anti-ageing and/orwound healing promoting action thereof is more pronounced).

The formulations according to the invention are preferably in the formof an emulsion, e.g. W/O (water-in-oil), O/W (oil-in-water), W/O/W(water-in-oil-in-water), O/W/O (oil-in-water-in-oil) emulsion, PITemulsion, Pickering emulsion, emulsion with a low oil content, micro- ornanoemulsion, a solution, e.g. in oil (fatty oils or fatty acid esters,in particular C₆-C₃₂ fatty acid C₂-C₃₀ esters) or silicone oil,dispersion, suspension, creme, lotion or milk, depending on theproduction method and ingredients, a gel (including hydrogel,hydrodispersion gel, oleogel), spray (e.g. pump spray or spray withpropellant) or a foam or an impregnating solution for cosmetic wipes, adetergent, e.g. soap, synthetic detergent, liquid washing, shower andbath preparation, bath product (capsule, oil, tablet, salt, bath salt,soap, etc.), effervescent preparation, a skin care product such as e.g.an emulsion (as described above), ointment, paste, gel (as describedabove), oil, balsam, serum, powder (e.g. face powder, body powder), amask, a pencil, stick, roll-on, pump, aerosol (foaming, non-foaming orpost-foaming), a deodorant and/or antiperspirant, mouthwash and mouthrinse, a foot care product (including keratolytic, deodorant), an insectrepellent, a sunscreen, aftersun preparation, a shaving product,aftershave balm, pre- and aftershave lotion, a depilatory agent, a haircare product such as e.g. shampoo (including 2-in-1 shampoo,anti-dandruff shampoo, baby shampoo, shampoo for dry scalps,concentrated shampoo), conditioner, hair tonic, hair water, hair rinse,styling creme, pomade, perm and setting lotion, hair spray, styling aid(e.g. gel or wax), hair smoothing agent (detangling agent, relaxer),hair dye such as e.g. temporary direct-dyeing hair dye, semi-permanenthair dye, permanent hair dye, hair conditioner, hair mousse, eye careproduct, make-up, make-up remover or baby product.

The formulations according to the invention are particularly preferablyin the form of an emulsion, in particular in the form of a W/O, O/W,W/O/W, O/W/O emulsion, PIT emulsion, Pickering emulsion, emulsion with alow oil content, micro- or nanoemulsion, a gel (including hydrogel,hydrodispersion gel, oleogel), a solution e.g. in oil (fatty oils orfatty acid esters, in particular C₆-C₃₂ fatty acid C₂-C₃₀ esters)) orsilicone oil, or a spray (e.g. pump spray or spray with propellant).

Auxiliary substances and additives can be included in quantities of 5 to99% b.w., preferably 10 to 80% b.w., based on the total weight of theformulation. The amounts of cosmetic or dermatological auxiliary agentsand additives and perfume to be used in each case can easily bedetermined by the person skilled in the art by simple trial and error,depending on the nature of the particular product.

The preparations can also contain water in a quantity of up to 99% b.w.,preferably 5 to 80% b.w., based on the total weight of the preparation.

Capsules and Micro-Capsules

For oral uptake, encapsulation of the extracts represents a preferredembodiment. Usually encapsulation can take place by using gelatine as amatrix. It is also possible to prepare capsules by adding a gellingagent such as, for example, alginate to the extracts and drop themixture into a bath of a calcium salt. Both methods lead tomacro-capsules having a diameter of from about 1 cm to about 5 cm whichare toxicologically safe and suitable for consumption.

It may also be desired to encapsulate the extracts for the formulationof compositions which are developed for topical application. This canhave different reasons: stabilisation against an interaction with othercompounds in the formulation, protection against chemical degradation orsimply for the preparation of a very aesthetical product. For thispurpose, usually microcapsules are applied. “Microcapsules” areunderstood to be spherical aggregates with a diameter of from about 0.1to about 5 mm which contain at least one solid or liquid core surroundedby at least one continuous membrane. More precisely, they are finelydispersed liquid or solid phases coated with film-forming polymers, inthe production of which the polymers are deposited onto the material tobe encapsulated after emulsification and coacervation or interfacialpolymerization. In another process, liquid active principles areabsorbed in a matrix (“microsponge”) and, as microparticles, may beadditionally coated with film-forming polymers. The microscopicallysmall capsules, also known as nanocapsules, can be dried in the same wayas powders. Besides single-core microcapsules, there are alsomultiple-core aggregates, also known as microspheres, which contain twoor more cores distributed in the continuous membrane material. Inaddition, single-core or multiple-core microcapsules may be surroundedby an additional second, third, etc., membrane. The membrane may consistof natural, semisynthetic or synthetic materials. Natural membranematerials are, for example, gum arabic, agar agar, agarose,maltodextrins, alginic acid and salts thereof, for example sodium orcalcium alginate, fats and fatty acids, cetyl alcohol, collagen,chitosan, lecithins, gelatin, albumin, shellac, polysaccharides, such asstarch or dextran, polypeptides, protein hydrolyzates, sucrose andwaxes. Semisynthetic membrane materials are inter alia chemicallymodified celluloses, more particularly cellulose esters and ethers, forexample cellulose acetate, ethyl cellulose, hydroxypropyl cellulose,hydroxypropyl methyl cellulose and carboxymethyl cellulose, and starchderivatives, more particularly starch ethers and esters. Syntheticmembrane materials are, for example, polymers such as polyacrylates,polyamides, polyvinyl alcohol or polyvinyl pyrrolidone. Examples ofknown microcapsules are the following commercial products (the membranematerial is shown in brackets) Hallcrest Microcapsules (gelatin, gumarabic), Coletica Thalaspheres (maritime collagen), Lipotec Millicapseln(alginic acid, agar agar), Induchem Unispheres (lactose,microcrystalline cellulose, hydroxypropylmethyl cellulose), Unicetin C30(lactose, microcrystalline cellulose, hydroxypropylmethyl cellulose),Kobo Glycospheres (modified starch, fatty acid esters, phospholipids),Softspheres (modified agar agar) and Kuhs Probiol Nanospheres(phospholipids).

Non-Pharmaceutical Applications

In addition, the invention is directed at a number of non-pharmaceuticalapplications, in particular to the use of the extracts of microalgae orhalophytes or psammophilous plants

-   -   for the treatment of human hair;    -   for the treatment of human skin;    -   for the treatment of the human genitals;    -   for modulating sebogenesis in human hair and/or human skin;    -   for improving the hair appearance, in particular for treating        greasy hair;    -   for preventing and treating scalp disorders connected with        excessive sebogenesesis, in particular for preventing and        treating dandruff;    -   for improving the skin appearance, in particular for treating        oily skin;    -   for preventing and treating skin disorders such as seborrhea,        acne vulgaris and comedones;    -   for modulating the sebogenesis in the human genital area and in        particular in the vulva.

All these applications can be summarized under the expression“modulation” of sebogenesis in human skin and hair, in order to fight orprevent symptoms like slight blemishes such as oily skin and greasyhair, and more important dysfunctions such as dandruff, comedones,pimples, pruritus vulvae, etc.

Pharmaceutical Applications

Additional objects of the present invention are related to medicaments,in particular:

An extract of

-   (i) a microalgae or-   (ii) a halophyte or-   (iii) a psammophilous plant    for use as a medicament.

Also covered by the present invention is an extract of

-   (iv) a microalgae or-   (v) a halophyte or-   (vi) a psammophilous plant    for use as a medicament for preventing or fighting    -   dysfunctions of human hair and/or skin.    -   scalp disorders connected with excessive sebogenesis;    -   dandruff;    -   seborrhea;    -   acne vulgaris;    -   comedones.

In the following, the invention is illustrated by—but not limitedto—various working examples.

EXAMPLES

Microalgae

The extraction protocols were selected from many other technicalsolutions, and they have to be considered as truly exemplificativerepresentations. According to the present invention, freeze-driedbiomasses of microalgae were extracted according to the protocolpreviously described, with a liquid extractant selected from the groupconsisting of ethyl acetate, isopropanol, ethanol, methanol and water.

The extractant can also comprise a mixture of two or more of theaforementioned solvents.

As already reported, the extract concentrations are expressed here asratio between the weights of dry biomass extracted and the volume ofextractant (μg/ml).

Description of the Experimental Model Based on Ex-Vivo Culture of HumanSebaceous Glands (hSGs) and Subsequent Quantification of their SebumContent

All the reported examples are intended to show the modulation of sebumproduction exerted by the experimental preparations on human hSGsmicrodissected and cultivated up to day 6. At the end of the culturetime, the sebum is extracted and quantified from each experimental groupof hSGs and then normalized by the proteins extracted from the residualhSG material (mg lipids/mg proteins). As a result, the biologicalactivity of the tested compounds is inferred by comparing the ratiolipids/proteins of the treated glands with that of the control group.

Organ Culture Technique

Using micro-scissors and tweezers, hSGs were isolated from thepilosebaceous units of a scalp skin sample. They were seeded in 24-wellplates at the density of 8 hSGs/well and then cultivated in 500 μl ofmodified William E medium. After 24 hours of culture the viability ofthe hSGs was assessed by means of resazurine assay. Briefly, each hSGsgroup was transferred onto a microplate well with 200 μl of 10%resazurin culture medium for 2 hours. During this period the resazurin,a non-fluorescent blue dye, is reduced by living cells to the pinkcoloured and highly red fluorescent resorufin. At the end of theincubation, the medium was withdrawn and analyzed for the resazurinfluorescence in a plate reader (Em. 570 nm-Ex. 590 nm). The fluorescencesignal positively correlates with the hSGs viability. Since theresazurin test is not toxic, the hSGs were then seeded in a 24-wellplate and cultivated with the experimental culture media in order tostart the treatments. The control received William E mediumappropriately modified, while the samples submitted to experimentaltreatments received the same medium supplemented with experimentalextracts. The culture medium was renewed every other day. After six daysof organ culture, the viability of the hSGs was again assessed viaresazurine assay and then, having attested their good viability, eachgroup of hGSs was collected and analyzed for quantifying the sebumcontent.

Analysis of the Sebum Content

In order to make the estimated productivity of the glands comparable,which are variable in biomass, their total sebum content was estimatedand divided by the proteins extracted from the gland tissue, obtainingthe ratio between the produced sebum and the tissue proteins (i.e. mg oflipids/mg of proteins).

The sebum extraction and quantification was performed as reported below:

Each hSG group was homogenized in 100 μl of isopropyl alcohol;

the sample was centrifuged at 14,000 G for 5 minutes and then thesupernatant (containing the extracted sebum) was collected;

the sebum extract was analyzed in triplicate with a Direct Detect IRSpectrometer (Millipore), which provided the total lipid concentrationof the supernatant (mg/ml);

the total lipids of the hSGs was quantified multiplying the supernatantlipid concentration (indention 3) by the volume of isopropyl alcoholadopted for the lipid extraction (indention 1);

the pellet remaining from indention 2 was dried by means of a vacuum dryevaporator and then again homogenized in 50 μl of proteolytic buffer (20mM Tris/HCl pH 7.5, 150 mM NaCl, 2 mM EDTA, 0.5% Triton X-100, 2 mM DTT,1% protease inhibitor cocktail);

after an appropriate incubation time, this extractive mixture wascentrifuged at 14,000 G for 10 minutes and the supernatant was collectedand analyzed in triplicate with a Direct Detect IR Spectrometer(Millipore);

the obtained total protein concentration was multiplied by theextractive volume (indention 5) in order to quantify the total proteinsof the hSGs;

the total lipid amount (indention 4), i.e. the amount of sebum, wasdivided by the total proteins (indention 7) in order to obtain thenormalized amount of lipids per mg of proteins (mg of lipids/mg ofproteins).

The amounts of normalized lipids obtained from the treated groups, i.e.the sebum produced by each group of hSGs, were expressed in percentageswith respect to the value obtained in the control group, in order topoint out the regulatory effect performed by the experimental treatment.

Examples 1 to 6

Activity of Ethanolic and Aqueous Extracts of Thalassiosira on HumanSebaceous Glands (hSGs)

hSGs were taken from a scalp sample and cultivated as previouslydescribed. Ethanolic and aqueous extracts obtained from Thalassiosirapseudonana were vacuum dried and then dissolved in DMSO at the finalconcentration 10,000 μg/ml. The experimental culture media weresupplemented with 1 μl/ml of these stock solutions in order to obtainthe experimental treatments at 10 μg/ml, while the lower concentrationswere obtained from these supplemented media by serial volumetricdilution 1:10 with standard medium. All the treatments were supplementedwith DMSO, whenever needed, to the final concentration of 1 μl/ml. Thecontrol group was cultured in standard medium supplemented with 1 μl/mlof DMSO. As positive control, a 5 μM Capsaicin treatment was included inthe experimental design. Capsaicin is an active component of chilipeppers suitable to inhibit sebogenesis [Tóth et al., J. Invest. Derm.(2009), 129: 329-339]. The results obtained from the experiments arereported in Table 2.

TABLE 2 Sebum content in hSGs following treatment with Thalassiosiraextracts. Responses are expressed as % ratio of the control groupperformance. The capsaicin treatment was included as positive control.The statistical significance was evaluated by means of one-way ANOVAPermutation test with Dunnett permutation post-hoc test Example SampleAmount Average Std. error Statistics 0 Control 0 100.0 1.4 0 capsaicin 5μM 90.3 1.8 p < 0.01 1 EtOH 0.1 μg/ml 50.2 1.3 p < 0.01 2 EtOH 1.0 μg/ml78.6 2.0 p < 0.01 3 EtOH 10.0 μg/ml 49.2 1.6 p < 0.01 4 Water 0.1 μg/ml51.8 1.1 p < 0.01 5 Water 1.0 μg/ml 50.4 1.1 p < 0.01 6 Water 10.0 μg/ml68.0 1.0 p < 0.01

The positive control treatment reduced the sebum content of the hSGs by10% in comparison with the control group. However, surprisingly, boththe Thalassiosira extracts produced an intense inhibition of thesebogenesis, ranging from 32% to 51% in comparison with the controlgroup.

All these results are highly significant on a statistical basis.

Examples 7 to 8

Activity of Ethanolic and Aqueous Extracts of Thalassiosira on HumanSebaceous Glands (hSGs)

The ethanolic and aqueous extracts tested in the previous experimentwere again tested at the single concentration of 0.1 μg/ml. No positivecontrol was included in this experimental design. The results arereported in Table 3:

TABLE 3 Sebum content in hSGs following treatment with Thalassiosiraextracts. Responses are expressed as % ratio of the control groupperformance. The statistical significance was evaluated by means ofone-way ANOVA Permutation test with Dunnett permutation post-hoc testExample Sample Amount Average Std. error Statistics 0 Control 0 100.02.0 7 EtOH 0.1 μg/ml 84.6 2.2 p < 0.01 8 Water 0.1 μg/ml 65.5 1.3 p <0.01

The results confirmed the intense inhibition of sebum production inducedby the treatments with extracts of Thalassiosira. In this case, at thetested concentration, the aqueous extract produced a more intenseinhibition than the ethanolic one.

Examples 9 to 13

Activity of Various Thalassiosira Extracts on Human Sebaceous Glands(hSGs)

The previously described experimental protocol was used to study theactivity of some extracts obtained from Thalassiosira pseudonana bymeans of different solvents: ethyl acetate (EtAc), ethanol (EtOH) andwater. The biological activity of these preparations was compared bytreating groups of hSGs microdissected from a single sample of scalp.

Organ culture and supplementation of the culture media were performed asreported for the previous experiments. This experimental design includedtwo different positive controls selected from among commercial compoundsactive on sebogenesis: 5α-Avocuta (Butyl-Avocadate), which is an activeingredient derived from avocado pears, and Asebiol™, a commercial activeproduct formulated combining aminoacids, sulphated peptides, vitamin Bcomplex and allantoin.

The variations of sebum content expressed by each group in comparison tothe control are reported in Table 4.

TABLE 4 Sebum content in hSGs following treatment with Thalassiosiraextracts obtained with ethyl acetate (EtAc), ethanol (EtOH) and water(Water). 5α-Avocuta (Butyl-Avocadate) and Asebiol ™ were included aspositive controls. Responses are expressed as % ratio of the controlgroup performance. The statistical significance was evaluated by meansof one-way ANOVA Permutation test with Dunnett permutation post-hoc testExample Sample Amount Average Std. error Statistics 0 Control (DMSO) 0100.0 1.0 0 5α-Avocuta 0.1% 82.4 1.6 P < 0.01 0 Asebiol ™ 0.1% 82.4 2.7P < 0.01 9 EtAc 0.1 μg/ml 92.2 1.3 P < 0.05 10 EtAc 1.0 μg/ml 77.1 0.6 P< 0.01 11 EtOH 0.1 μg/ml 87.1 2.3 P < 0.01 12 EtOH 1.0 μg/ml 80.5 1.3 P< 0.01 13 Water 0.1 μg/ml 81.4 2.0 P < 0.01

The results obtained attest that all the experimental preparationsinhibited the production of sebum in measures comparable to or higherthan the positive controls. In fact, the sebum content of the hSGstreated with Thalassiosira extracts was from 7.8% to 22.9% lower thanthe control group, while both the commercial products reduced the sebumcontent by 17.6%. All the extracts produced significant (P<0.05) or verysignificant (P<0.01) inhibitions on a statistical basis.

Examples 14 to 19

Activity on Human Sebaceous Glands (hSGs) of Ethanolic Extracts Obtainedfrom Microalgae Belonging to the Genera Chlorococcum, Chaetoceros andMonodus

The experimental protocol previously described was adopted to study theactivity of ethanolic extracts obtained from microalgae belonging to thegenera Chlorococcum (C), Chaetoceros (K) and Monodus (M). For thepresent example, in particular, the ethanolic extracts (EtOH) wereprepared from Chorococcum minutum, Chaetoceros calcitrans f. pumilus andMonodus subterraneus. A culture medium supplemented with 5 μM capsaicinwas included in the experimental design as positive control.

After 6 days of culture and 5 of treatment, as previously described, thesebum content was estimated in each group of hSGs and the detectedvariations in comparison to the control are reported in Table 5.

TABLE 5 Sebum content in hSGs following treatment with ethanolicextracts (EtOH) obtained from Cholorococcum minutum (C), Chaetoceroscalcitrans f. pumilus (K) and Monodus subterraneus (M). Capsaicintreatment was included as positive control. Responses are expressed as %ratio of the control group performance. The statistical significance wasevaluated by means of one-way ANOVA Permutation test with Dunnettpermutation post-hoc test Example Sample Amount Average Std. errorStatistics 0 Control (DMSO) 0 100.0 1.7 0 Capsaicin 0 68.5 1.5 P < 0.0114 K - EtOH 0.1 μg/ml 60.6 2.3 P < 0.01 15 K - EtOH 10 μg/ml 59.3 1.2 P< 0.01 16 M - EtOH 0.1 μg/m 71.3 2.3 P < 0.01 17 M - EtOH 10 μg/ml 65.41.3 P < 0.01 18 C - EtOH 0.1 μg/ml 54.1 1.0 P < 0.01 19 C - EtOH 10μg/ml 53.6 0.3 P < 0.01

The results, surprisingly, attest that the screened microalgal extractsexert a significant inhibitory action on the sebum production by hSGs,generally more intense than that shown by the positive control(Capsaicin). All the extracts produced a reduction in sebum contentranging between 29% (Monodus 0.1 μg/ml) and 46% (Chlorococcum 0.1-10μg/ml). All the detected responses are highly significant on astatistical basis.

Examples 20 to 25

Activity on Human Sebaceous Glands (hSGs) of Ethanolic Extracts Obtainedfrom Microalgae Belonging to the Genera Chlorococcum, Chaetoceros andMonodus

The previous experiment was replicated with hSGs taken from a differentdonor. The results are reported in Table 6:

TABLE 6 Sebum content in hSGs following treatment with ethanolicextracts (EtOH) obtained from Cholorococcum minutum (C), Chaetoceroscalcitrans f. pumilus (K) and Monodus subterraneus (M). Capsaicintreatment was included as positive controls. Responses are expressed as% ratio of the control group performance. The statistical significancewas evaluated by means of one-way ANOVA Permutation test with Dunnettpermutation post-hoc test Example Sample Amount Average Std. errorStatistics 0 Control (DMSO) 0 100.0 1.1 0 Capsaicin 0 59.2 0.7 P < 0.0120 K - EtOH 0.1 μg/ml 58.0 1.2 P < 0.01 21 K - EtOH 10 μg/ml 59.2 0.9 P< 0.01 22 M - EtOH 0.1 μg/ml 67.9 0.9 P < 0.01 23 M - EtOH 10 μg/ml 52.80.6 P < 0.01 24 C - EtOH 0.1 μg/ml 56.1 0.5 P < 0.01 25 C - EtOH 10μg/ml 64.8 0.9 P < 0.01The results confirmed the intense inhibiting activity of theexperimental extracts on sebogenesis. All the extracts produced areduction in sebum content ranging between 32% (Monodus 0.1 μg/ml) and47% (Monodus 10 μg/ml). All the detected responses are highlysignificant on a statistical basis.

Examples 26 to 29

Activity on Human Sebaceous Glands (hSGs) of Aqueous Extracts Obtainedfrom Microalgae Belonging to the Genera Monodus and Chaetoceros

The protocol used for the previous experiment was adopted for screeningthe biological activity of aqueous extracts obtained from Monodussubterraneous and Chorococcum minutum. In this case, the concentratedaqueous extracts were used directly to supplement the experimentalculture media, without the addition of DMSO as intermediate vehicle. Thetreatment results are reported in Table 7:

TABLE 7 Sebum content in hSGs following treatment with aqueous extracts(water) obtained from Monodus subterraneous (M) and Chlorococcum minutum(C). Capsaicin treatment was included as positive control. Responses areexpressed as % ratio of the control group performance. The statisticalsignificance was evaluated by means of one-way ANOVA Permutation testwith Dunnett permutation post-hoc test Example Sample Amount AverageStd. error Statistics 0 Control (DMSO) 0 100.0 0.9 0 Capsaicin 0 97.41.0 n.s. 26 M - water 0.1 μg/ml 95.8 1.3 P < 0.05 27 M - water 10 μg/ml91.2 0.8 P < 0.01 28 C - water 0.1 μg/ml 91.3 1.1 P < 0.01 29 C - water10 μg/ml 80.2 1.2 P < 0.01The aqueous extracts resulted suitable to inhibit the sebum productionby hSGs. The tested donor resulted poorly responsive, as attested by thelow inhibition produced by the treatment with the positive control(−3%). Nevertheless, all the experimental preparations inhibited thesebum production in a statistically significant (P<0.05) or verysignificant (P>0.01) measure.

B. Terrestrial Plants

As for microalgae, the extraction protocols were selected from manyother technical solutions, and have to be considered as purelyexemplificative representations. According to the present invention,freshly harvested plants were minced and extracted with a liquidextractant selected from the group consisting of ethyl acetate,isopropanol, ethanol, methanol and water. The extractant can alsocomprise a mixture of two or more of these solvents.

In the following examples, differently from the conventionalconcentration adopted for the microalgae extracts, the extractconcentration was expressed as actual content of dry weight per volumeunit.

Examples 30 to 31

Activity on Human Sebaceous Glands (hSGs) of Water Extract Obtained fromPsammophilous Plants Belonging to the Genus Echinophora.

The previously described experimental protocol was adopted to study theactivity of the aqueous extract obtained from plants belonging to thegenus Echinophora. For the present example, in particular, the aqueousextract was prepared from Echinophora spinosa (ES), a typical plantgrowing on sand dunes along the Mediterranean coasts. A culture mediumsupplemented with 5 μM capsaicin was included in the experimental designas positive control.

After 6 days of culture and 5 of treatment, as previously described, thesebum content was estimated in each group of hSGs and the results arereported in Table 6.

TABLE 8 Sebum content in hSGs following treatment with aqueous extract(water) obtained from Echinophora spinosa (ES). Capsaicin treatment wasincluded as positive control. Responses are expressed as % ratio of thecontrol group performance. The statistical significance was evaluated bymeans of one-way ANOVA Permutation test with Dunnett permutationpost-hoc test Example Sample Amount Average Std. error Statistics 0Control 0 100.0 1.8 0 Capsaicin 0 91.9 1.5 P < 0.05 30 ES - water 0.1μg/ml 82.8 1.2 P < 0.01 31 ES - water 10 μg/ml 87.5 1.8 P < 0.01

The aqueous extract obtained from Echinophora spinosa inhibited thesebum production by 13.2-17.5%, i.e. 1.5-2 fold the inhibition inducedby the positive control. This effect has to be regarded as verysignificant based on the statistical analysis used.

Examples 32 to 40

Activity on Human Sebaceous Glands (hSGs) of Various Extracts Obtainedfrom Plants Belonging to the Genera Echinophora, Inula, Sarcocornia andSalicornia.

The previously described experimental protocol was adopted to study theactivity of the extracts obtained from plants belonging to the generaEchinophora, Inula, Sarcocornia and Salicornia. For the present example,an ethanolic extract was prepared from the psammophilous plantEchinophora spinosa (ES), whereas ethanolic and aqueous extracts wereprepared from Inula chritmoides (IC), a typical plant growing on sanddunes as well as in salty soils. Methanolic extracts were also preparedfrom two halophytes typical of Mediterranean salt marshes: Sarcocorniafruticosa (SF) and Salicornia veneta (SV).

After 6 days of culture and 5 of treatment, as previously described, thesebum content was estimated in each group of hSGs and the results arereported in Table 9.

TABLE 9 Sebum content in hSGs following treatment with ethanolic extract(EtOH) and aqueous extract (water) obtained from Inula chritmoides (IC)and Echinophora spinosa (ES), methanolic extracts (MeOH) obtained fromSarcocornia fruticosa (SF) and Salicornia veneta (SV). Capsaicintreatment was included as positive control. Responses are expressed as %ratio of the control group performance. The statistical significance wasevaluated by means of one-way ANOVA Permutation test with Dunnettpermutation post-hoc test Example Sample Amount Average Std. errorStatistics 0 Control 0 100.0 3.1 32 ES - EtOH 0.1 μg/ml 114.0 2.9 P <0.01 33 ES - EtOH 10 μg/ml 101.9 2.9 n.s. 34 IC - EtOH 10 μg/ml 71.8 1.1P < 0.01 35 IC - water 0.1 μg/ml 87.5 1.9 P < 0.01 36 IC - water 10μg/ml 80.3 1.4 P < 0.01 37 SF - MeOH 0.1 μg/ml 86.3 1.0 P < 0.01 38 SF -MeOH 10 μg/ml 76.1 1.9 P < 0.01 39 SV - MeOH 0.1 μg/ml 78.8 1.3 P < 0.0140 SV - MeOH 10 μg/ml 73.6 1.6 P < 0.01

Most of the treatments produced a significant decrease of sebumproduction, ranging between −13% and −28% in comparison with the controlgroup. These effects are very significant based on the statisticalanalysis used. Interestingly, the ethanolic extract of Echinophoraproduced a significant stimulation of sebogenesis at 0.1 μg/ml. Sincethe water extract of this plant produced a sebum decrease (see examples30-31), it is assumable that the stimulating active is a lipophiliccompound.

Examples 41 to 44

Activity on Human Sebaceous Glands (hSGs) of Ethanol Extracts Obtainedfrom Sarcocornia and Salicornia.

The previously described experimental protocol was adopted to study theactivity of the ethanolic extracts obtained from plants belonging to thegenera Sarcocornia and Salicornia. For the present experiment,Sarcocornia fruticosa (SF) and Salicornia veneta (SV) were selected asexemplificative species.

After 6 days of culture and 5 of treatment, as previously described, thesebum content was estimated in each group of hSGs and the results arereported in Table 10.

TABLE 10 Sebum content in hSGs following treatment with ethanolicextract (EtOH) obtained from Sarcocomia fruticosa (SF) and Salicomiaveneta (SV). Capsaicin treatment was included as positive control.Responses are expressed as % ratio of the control group performance. Thestatistical significance was evaluated by means of one-way ANOVAPermutation test with Dunnett permutation post-hoc test Example SampleAmount Average Std. error Statistics 0 Control 0 100.0 0.8 0 Capsaicin 5μg/ml 62.9 0.4 P < 0.01 41 SF - EtOH 0.1 μg/ml 91.8 1.2 P < 0.01 42 SF -EtOH 10 μg/ml 83.1 1.0 P < 0.01 43 SV - EtOH 0.1 μg/ml 60.4 0.3 P < 0.0144 SV - EtOH 10 μg/ml 92.3 0.8 P < 0.01

All the treatments produced a significant decrease of sebum production,ranging between −8% and −40% in comparison with the control group. Theseeffects are very significant based on the statistical analysis used.

Examples 45 to 53

Activity on Human Sebaceous Glands (hSGs) of Various Extracts Obtainedfrom Sarcocornia, Salicornia, Echinophora and Chaetoceros.

The previously described experimental protocol was adopted to study theactivity of the aqueous and ethanolic extracts obtained from thefollowing plants and microalgae selected as exemplificative species:Sarcocornia fruticosa (SF), Salicornia veneta (SV), Echinophora spinosa(ES) and Chaetoceros calcitrans (K).

After 6 days of culture and 5 of treatment, as previously described, thesebum content was estimated in each group of hSGs and the results arereported in Table 11.

TABLE 11 Sebum content in hSGs following treatment with ethanolic (EtOH)or aqueous (water) extracts obtained from Sarcocomia fruticosa (SF),Salicomia veneta (SV), Echinophora spinosa (ES) and Chaetoceroscalcitrans (K). Responses are expressed as % ratio of the control groupperformance. The statistical significance was evaluated by means ofone-way ANOVA Permutation test with Dunnett permutation post-hoc testExample Sample Amount Average Std. error Statistics 0 Control 0 100.01.4 0 SF - water 0.1 μg/ml 116.7 4.3 P < 0.01 45 SF - water 10 μg/ml106.6 3.4 n.s. 46 SV - water 0.1 μg/ml 88.1 2.8 P < 0.05 47 SV - water10 μg/ml 95.4 2.3 n.s. 48 SV - EtOH 0.1 μg/ml 81.8 1.4 P < 0.01 49 SV -EtOH 10 μg/ml 83.7 1.5 P < 0.01 50 ES - EtOH 0.1 μg/ml 155.6 5.3 P <0.01 51 ES - EtOH 10 μg/ml 123.8 1.3 P < 0.01 52 K - water 0.1 μg/ml132.2 2.5 P < 0.01 53 K - water 10 μg/ml 106.9 2.4 n.s.All the treatments produced significant responses, at least for one ofthe two tested concentrations. Both the acqueous and ethanolic extractsobtained from Salicornia veneta inhibited the sebum production, whereasall the other extracts induced the opposite response, i.e. stimulatedthe sebum production. These data attest that from Sarcocornia fruticosa,Echinophora spinosa and Chaetoceros calcitrans, it is possible to obtainextracts with opposite effects depending on the solvent adopted for theextract preparation.

CONCLUSIVE REMARKS

The reported examples attest that the selected microalgae, halophytesand psammophilous plants are suitable sources of natural extracts forthe regulation of sebum production. Their biological activity was shownto be comparable to or higher than that of some positive controlsselected from among the well-known sebum-inhibitors (i.e. 5α-Avocuta,Asebiol™, Capsaicin).

The described results support the proposed uses of the extracts to treatskin, hair and genitals, in order to prevent and/or treat the excessivesecretion of sebum and the related aesthetic problems or skin disorders(greasy hair and skin, dandruff, acne, discomfort of the vulval regionetc.).

What claimed is:
 1. A method for making and using an extract ofmicroalgae comprising the steps of (a) contacting each gram of plantmaterial, optionally minced or crushed or micronized, with 4 ml of asolvent selected from the group consisting of C₁-C₄ aliphatic alcohols,ethyl acetate, water and mixtures thereof, and causing active agent inthe plant material to move into the solvent phase, optionally atelevated temperatures, (b) removing the dissolved extract from theresidue, (c) recovering the extract from the solvent, and (d) topicallyor orally administering the extract of microalgae for the regulation ofsebum production by sebaceous glands to a patient in need of scalptreatment, treatment for greasy hair, dandruff treatment, treatment forseborrheic dermatitis, treatment of oily skin, treatment for comedones,and treatment of external female genitalia thereof, wherein the extractof microalgae belongs to the genus Chaetoceros, Chlorococcum,Thalassiosira, or Monodus.
 2. The method according to claim 1,additionally comprising combining the extract with a cosmeticallyacceptable carrier selected from the group consisting of C₁-C₄ aliphaticalcohols, polyols having 3 to 12 carbon atoms, oil components, water andmixtures thereof.
 3. The method according to claim 1, comprisingadditionally preventing and treating acne with the extract ofmicroalgae.
 4. The method according to claim 1, wherein the microalgaeis Bacillariophyceae belonging to the genus of Chaetoceros andThalassiosira.
 5. The method according to claim 4, wherein themicroalgae belongs to the genus of Chaetoceros.